Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T77913
|
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Former ID |
TTDS00086
|
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Target Name |
Histamine H1 receptor
|
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Gene Name |
HRH1
|
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Synonyms |
H1 Histamine receptor; Histamine receptor 1; HRH1
|
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Target Type |
Successful
|
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Disease | Anesthesia [ICD9: 338; ICD10: R20.0] | ||||
Allergic skin disorders [ICD10: L00-L99] | |||||
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | |||||
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | |||||
Allergic conjunctivitis [ICD9: 204.0, 372.0, 372.14, 995.3; ICD10: C91.0, H10, H10.45, T78.4] | |||||
Allergic disorders; Itching; Nausea [ICD9: 698, 787, 787.0, 995.3; ICD10: L29, R11, T78.4] | |||||
Allergic rhinitis; Urticaria [ICD9: 477, 708; ICD10: J30, L50] | |||||
Allergy [ICD9: 995.3; ICD10: T78.4] | |||||
Asthma [ICD10: J45] | |||||
Anxiety disorder; Morning sickness [ICD9: 300, 643.0; ICD10: F40-F42, O21.0] | |||||
Allergic rhinitis; Urticaria; Pruritus [ICD9: 477, 708; ICD10: J30, L50] | |||||
Common cold; Allergies [ICD9: 460, 995.3; ICD10: J00, T78.4] | |||||
Dry cough [ICD10: R05] | |||||
Depression [ICD9: 311; ICD10: F30-F39] | |||||
Hypersensitivity reactions; Coughs; Common colds [ICD10: R05] | |||||
Hay fever [ICD9: 477; ICD10: J30] | |||||
Hay fever; Allergic rhinitis [ICD9:477, 472.0, 995.3; ICD10: J30, J00, J31.0, T78.4] | |||||
Hay fever; Cough [ICD9:477, 786.2; ICD10: J30, R05] | |||||
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0] | |||||
Insomnia; Anxiety disorder [ICD9:307.41, 307.42, 327.0, 780.51, 780.52, 300, 311; ICD10: F51.0, G47.0, F32, F40-F42] | |||||
Nasal congestion [ICD9: 478.19; ICD10: J34.89] | |||||
Nausea; Vomiting [ICD9: 787, 787.0; ICD10: R11] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Ocular allergy [ICD9: 360-379; ICD10: H00-H59] | |||||
Pruritus [ICD9: 698; ICD10: L29] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Parkinson's disease [ICD9: 332; ICD10: G20] | |||||
Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis [ICD10: H10] | |||||
Respiratory allergies; Allergic rhinitis [ICD9:460-519, 472.0, 477, 995.3; ICD10: J00-J99, J00, J30, J31.0, T78.4] | |||||
Respiratory allergies; Cancer [ICD9:460-519, 140-229; ICD10: J00-J99, C00-C96] | |||||
Rhinitis [ICD9: 472.0, 477; ICD10: J00, J30, J31.0] | |||||
Respiratory disease [ICD10: J00-J99] | |||||
Rhinitis; Urticaria; Allergy [ICD10: J00, J30, J31.0, L50, T78.4] | |||||
Sleep disorders [ICD9: 307.4, 327, 780.5; ICD10: F51, G47] | |||||
Seasonal and perennial allergic rhinitis and vasomotor rhinitis [ICD10: J30] | |||||
Vertigo meniere's disease [ICD9: 386.0, 438.85, 780.4; ICD10: H81, H81.0, R42] | |||||
Vertigo's disease; Meniere's disease [ICD10: H81.09] | |||||
Unspecified [ICD code not available] | |||||
Function |
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
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BioChemical Class |
GPCR rhodopsin
|
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Target Validation |
T77913
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UniProt ID | |||||
Sequence |
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK RILHIRS |
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Drugs and Mode of Action | |||||
Drug(s) | (S)-(+)-Dimethindene maleate | Drug Info | Approved | Pruritus | [535933] |
Aceprometazine | Drug Info | Approved | Sleep disorders | [550730] | |
Acrivastine | Drug Info | Approved | Allergic rhinitis | [534869] | |
Alcaftadine | Drug Info | Approved | Allergic conjunctivitis | [531351], [542577] | |
Antazoline | Drug Info | Approved | Nasal congestion | [538515], [542123] | |
Azatadine | Drug Info | Approved | Allergic rhinitis | [538492], [542126] | |
Azelastine | Drug Info | Approved | Allergic conjunctivitis | [536119], [542129] | |
Bepotastine | Drug Info | Approved | Allergic rhinitis; Urticaria; Pruritus | [536119], [542491] | |
Bromodiphenhydramine | Drug Info | Approved | Hay fever; Cough | [538416], [542139], [551871] | |
Brompheniramine | Drug Info | Approved | Allergic rhinitis | [538351], [542140] | |
Buclizine | Drug Info | Approved | Nausea; Vomiting | [542141], [550717] | |
Carbinoxamine | Drug Info | Approved | Seasonal and perennial allergic rhinitis and vasomotor rhinitis | [551871] | |
Cetirizine | Drug Info | Approved | Allergic rhinitis | [534869], [538734] | |
Chlophedianol | Drug Info | Approved | Dry cough | [551871] | |
Chlorpheniramine | Drug Info | Approved | Allergic rhinitis; Urticaria | [538228], [542007] | |
Cinnarizine | Drug Info | Approved | Vertigo meniere's disease | [550678] | |
Clemastine | Drug Info | Approved | Allergic rhinitis | [538250], [541312] | |
Cyclizine | Drug Info | Approved | Nausea; Vomiting | [538421], [542159] | |
Cyproheptadine | Drug Info | Approved | Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis | [551871] | |
Desloratadine | Drug Info | Approved | Allergic rhinitis | [536542], [542165] | |
Dexbrompheniramine | Drug Info | Approved | Hay fever; Allergic rhinitis | [538375], [542578], [551871] | |
Dexchlorpheniramine Maleate | Drug Info | Approved | Rhinitis; Urticaria; Allergy | [551871] | |
Dimenhydrinate | Drug Info | Approved | Nausea; Vomiting | [538185] | |
Dimethindene | Drug Info | Approved | Respiratory allergies; Allergic rhinitis | [535933], [551871] | |
Diphenhydramine | Drug Info | Approved | Vertigo's disease; Meniere's disease | [551871] | |
Diphenylpyraline | Drug Info | Approved | Allergic rhinitis | [542174], [550716] | |
Doxepin | Drug Info | Approved | Depression | [536306], [538737] | |
Doxylamine | Drug Info | Approved | Anxiety disorder; Morning sickness | [538170], [542181] | |
Emedastine | Drug Info | Approved | Allergic conjunctivitis | [536119], [542184] | |
Epinastine | Drug Info | Approved | Allergic conjunctivitis | [536119], [542186] | |
Ergotidine | Drug Info | Approved | Respiratory allergies; Cancer | [535111], [538761], [551871] | |
Ethopropazine | Drug Info | Approved | Parkinson's disease | [536923], [542192] | |
Fexofenadine | Drug Info | Approved | Allergic rhinitis | [468050], [534869] | |
Hydroxyzine | Drug Info | Approved | Anxiety disorder | [538358], [542211] | |
Ketotifen | Drug Info | Approved | Allergic conjunctivitis | [536119], [542220] | |
Levocabastine | Drug Info | Approved | Allergic conjunctivitis | [536119], [538963] | |
Levocetirizine dihydrochloride | Drug Info | Approved | Allergic rhinitis | [538587], [538725] | |
Loratadine | Drug Info | Approved | Allergy | [536542], [542231] | |
Mepyramine | Drug Info | Approved | Allergy | [537515], [538732] | |
Mepyramine maleate | Drug Info | Approved | Allergy | [537515] | |
Mequitazine | Drug Info | Approved | Allergic rhinitis | [550725] | |
Methdilazine | Drug Info | Approved | Allergic rhinitis | [542247], [550689] | |
Mizolastine | Drug Info | Approved | Allergic rhinitis | [535216] | |
Olopatadine | Drug Info | Approved | Allergic conjunctivitis | [536119], [542266] | |
Oxatomide | Drug Info | Approved | Hay fever | [536700] | |
Pemirolast | Drug Info | Approved | Allergic conjunctivitis | [536119], [542352], [551871] | |
Phenindamine | Drug Info | Approved | Common cold; Allergies | [550767] | |
Pheniramine | Drug Info | Approved | Hay fever | [536119], [542286] | |
Promethazine | Drug Info | Approved | Allergic disorders; Itching; Nausea | [538374], [542302] | |
Propiomazine | Drug Info | Approved | Insomnia; Anxiety disorder | [538458], [542304], [551871] | |
Pyrilamine Maleate | Drug Info | Approved | Headache | [536700], [537884] | |
Tranilast | Drug Info | Approved | Ocular allergy | [536119], [541472] | |
Trimeprazine | Drug Info | Approved | Allergic rhinitis | [542253], [550775] | |
Tripelennamine | Drug Info | Approved | Hypersensitivity reactions; Coughs; Common colds | [551871] | |
Triprolidine | Drug Info | Approved | Hay fever | [536361], [538740] | |
RUPATADINE | Drug Info | Phase 4 | Discovery agent | [521763] | |
AC-170 | Drug Info | Phase 3 | Allergic conjunctivitis | [524743] | |
Carebastine | Drug Info | Phase 3 | Ocular allergy | [536119] | |
Olopatadine | Drug Info | Phase 3 | Ocular allergy | [536119], [542266] | |
E-4716 | Drug Info | Phase 2 | Respiratory disease | [527345] | |
LY-2624803 | Drug Info | Phase 2 | Insomnia | [522475] | |
Noberastine | Drug Info | Phase 2 | Asthma | [544807] | |
OBE-101 | Drug Info | Phase 2 | Obesity | [521932] | |
UCB-35440 | Drug Info | Phase 2 | Rhinitis | [549930] | |
Vapitadine | Drug Info | Phase 2 | Allergic skin disorders | [547977] | |
Astemizole | Drug Info | Withdrawn from market | Allergic rhinitis | [534869], [539680] | |
Chlophedianol | Drug Info | Withdrawn from market | Anesthesia | [542347], [550773] | |
Terfenadine | Drug Info | Withdrawn from market | Allergy | [534869], [539685] | |
Norastemizole | Drug Info | Discontinued in Preregistration | Discovery agent | [546280] | |
GSK835726 | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [548731] | |
HSR-609 | Drug Info | Discontinued in Phase 2 | Rhinitis | [545924] | |
Loratadine | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [547333] | |
Mequitamium iodide | Drug Info | Discontinued in Phase 2 | Asthma | [544538] | |
ReN-1869 | Drug Info | Discontinued in Phase 2 | Pain | [547211] | |
SUN-1334H | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [548589] | |
AZD-1744 | Drug Info | Discontinued in Phase 1 | Asthma | [548471] | |
GSK1004723 | Drug Info | Discontinued in Phase 1 | Allergic rhinitis | [548732] | |
KA-398 | Drug Info | Terminated | Asthma | [546278] | |
Selenotifen | Drug Info | Terminated | Asthma | [544859] | |
SUN-1334H | Drug Info | Investigative | Unspecified | [529341] | |
Antagonist | (+)-cis-H2-PAT | Drug Info | [526358] | ||
(+)-trans-H2-PAT | Drug Info | [526358] | |||
(+/-)-cis-H2-PAT | Drug Info | [526358] | |||
(+/-)-trans-H2-PAT | Drug Info | [526358] | |||
(-)-trans-H2-PAT | Drug Info | [526358] | |||
(S)-(+)-Dimethindene maleate | Drug Info | [535859], [535933], [537168], [537884] | |||
(S)-cetirizine | Drug Info | [527113] | |||
9-OH-risperidone | Drug Info | [534281] | |||
AC-170 | Drug Info | [551442] | |||
Aceprometazine | Drug Info | [536284] | |||
Acrivastine | Drug Info | [534875], [537691] | |||
Alcaftadine | Drug Info | [531351] | |||
Antazoline | Drug Info | [534867], [535973], [537070], [537691] | |||
arpromidine | Drug Info | [526569] | |||
Astemizole | Drug Info | [537070], [537328] | |||
Azatadine | Drug Info | [537651] | |||
Azelastine | Drug Info | [536700], [537714] | |||
Bepotastine | Drug Info | [536767] | |||
Bromodiphenhydramine | Drug Info | [537648] | |||
Brompheniramine | Drug Info | [537912] | |||
BU-E 47 | Drug Info | [526569] | |||
Buclizine | Drug Info | [535805] | |||
Carbinoxamine | Drug Info | [537829] | |||
Carebastine | Drug Info | [536119] | |||
Cetirizine | Drug Info | [535660], [537488] | |||
Chlophedianol | Drug Info | [537715] | |||
Chlorpheniramine | Drug Info | [534934], [536700], [537884] | |||
Cinnarizine | Drug Info | [534845], [535477] | |||
Clemastine | Drug Info | [536618], [536744] | |||
Cyclizine | Drug Info | [535368], [535716], [537890] | |||
Cyproheptadine | Drug Info | [536089], [536720] | |||
Desloratadine | Drug Info | [537072], [537098] | |||
Dexbrompheniramine | Drug Info | [538137] | |||
Dimenhydrinate | Drug Info | [535364], [536878] | |||
Dimethindene | Drug Info | [535859], [535933], [537168], [537884] | |||
Diphenhydramine | Drug Info | [534958], [536700] | |||
Diphenylpyraline | Drug Info | [537891] | |||
Doxylamine | Drug Info | [536000], [536430] | |||
Emedastine | Drug Info | [537537] | |||
Epinastine | Drug Info | [537248] | |||
Fexofenadine | Drug Info | [535660], [537072] | |||
GSK1004723 | Drug Info | [550963] | |||
GSK835726 | Drug Info | [550963] | |||
HSR-609 | Drug Info | [534391], [551871] | |||
Hydroxyclemastine | Drug Info | [536618], [536744] | |||
Hydroxyzine | Drug Info | [536846], [536963] | |||
impromidine | Drug Info | [527955] | |||
Ketotifen | Drug Info | [535339], [536700] | |||
Levocabastine | Drug Info | [535848], [536800] | |||
Levocetirizine dihydrochloride | Drug Info | [535339], [536700], [537072] | |||
Loratadine | Drug Info | [537347], [538066], [538157] | |||
Mepyramine | Drug Info | [537488], [537502], [537515] | |||
Mepyramine maleate | Drug Info | [537488], [537502], [537515] | |||
Mequitazine | Drug Info | [536811] | |||
Methdilazine | Drug Info | [537703] | |||
Mizolastine | Drug Info | [536717] | |||
Noberastine | Drug Info | [528242] | |||
Olopatadine | Drug Info | [536119] | |||
Oxatomide | Drug Info | [535848], [536700] | |||
Pemirolast | Drug Info | [536707] | |||
Phenindamine | Drug Info | [537846] | |||
Pheniramine | Drug Info | [535251] | |||
Promethazine | Drug Info | [536700], [537884] | |||
Propiomazine | Drug Info | [536316] | |||
Pyrilamine Maleate | Drug Info | [536700], [537884] | |||
ReN-1869 | Drug Info | [526246] | |||
SUN-1334H | Drug Info | [529341] | |||
Terfenadine | Drug Info | [536727], [538157] | |||
Tranilast | Drug Info | [536119] | |||
Trimeprazine | Drug Info | [536153] | |||
Tripelennamine | Drug Info | [535112], [535869], [536003], [536086] | |||
Triprolidine | Drug Info | [536896] | |||
Vapitadine | Drug Info | [547978] | |||
[11C]doxepin | Drug Info | [527045] | |||
[11C]pyrilamine | Drug Info | [543664] | |||
Inhibitor | 1-(4-p-Tolyl-butyl)-piperidine | Drug Info | [530299] | ||
1-[(Furan-2(5H)-one)-4-methyl]-desloratadine | Drug Info | [530666] | |||
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine | Drug Info | [530331] | |||
3,3-diphenylpropan-1-amine | Drug Info | [530331] | |||
4,4-Diphenylbutan-1-amine | Drug Info | [530331] | |||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | |||
9-(2-aminoethyl)-9,10-dihydroanthracene | Drug Info | [530331] | |||
9-(2-aminopropyl)-9,10-dihydroanthracene | Drug Info | [530331] | |||
9-(Aminomethyl)-9,10-dihydroanthracene | Drug Info | [530331] | |||
9-Phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine | Drug Info | [525803] | |||
DIMEBOLIN | Drug Info | [530547] | |||
Diphenyl(piperidin-4-yl)methanol | Drug Info | [530299] | |||
Doxepin | Drug Info | [536469] | |||
KF-A6 | Drug Info | [529032] | |||
MDL-28163 | Drug Info | [527799] | |||
N,N-dimethyl-2,2-diphenylethanamine | Drug Info | [530331] | |||
N,N-Dimethyl-3,3-diphenylpropan-1-amine | Drug Info | [530331] | |||
N,N-dimethyl-4,4-diphenylbutan-1-amine | Drug Info | [530331] | |||
N-hydroxycarbamate derivative | Drug Info | [527411] | |||
N-methyl-3,3-diphenylpropan-1-amine | Drug Info | [530331] | |||
N-methyl-4,4-diphenylbutan-1-amine | Drug Info | [530331] | |||
OCTOCLOTHEPIN | Drug Info | [531171] | |||
R-226161 | Drug Info | [528772] | |||
R-dimethindene | Drug Info | [530300] | |||
RUPATADINE | Drug Info | [527799] | |||
VUF-10148 | Drug Info | [529387] | |||
Agonist | 2-(2-thiazolyl)ethanamine | Drug Info | [526569] | ||
2-(3-bromophenyl)histamine | Drug Info | [526569] | |||
2-(3-chlorophenyl)histamine | Drug Info | [526569] | |||
2-(3-iodophenyl)histamine | Drug Info | [526569] | |||
2-pyridylethylamine | Drug Info | [527113] | |||
8R-Lisuride | Drug Info | [535914] | |||
dimethylhistaprodifen | Drug Info | [526569] | |||
Ergotidine | Drug Info | [535111] | |||
histaprodifen | Drug Info | [527589] | |||
methylhistaprodifen | Drug Info | [526569] | |||
oxo-arpromidine | Drug Info | [527955] | |||
S-(-)-Lisuride | Drug Info | [535914] | |||
UR-PG131A | Drug Info | [527955] | |||
UR-PG146 | Drug Info | [527955] | |||
UR-PG153 | Drug Info | [527955] | |||
UR-PG55B | Drug Info | [527955] | |||
Modulator | AZD-1744 | Drug Info | [1572591] | ||
Dexchlorpheniramine Maleate | Drug Info | [556264] | |||
E-4716 | Drug Info | [527345] | |||
Ethopropazine | Drug Info | [556264] | |||
KA-398 | Drug Info | [543664] | |||
LY-2624803 | Drug Info | [533039] | |||
Mequitamium iodide | Drug Info | [531768] | |||
Norastemizole | Drug Info | ||||
OBE-101 | Drug Info | [544069] | |||
Selenotifen | Drug Info | [527929] | |||
UCB-35440 | Drug Info | [527359] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Inflammatory mediator regulation of TRP channels | |||||
PANTHER Pathway | Histamine H1 receptor mediated signaling pathway | ||||
Reactome | Histamine receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | Monoamine GPCRs | ||||
GPCRs, Class A Rhodopsin-like | |||||
IL-4 Signaling Pathway | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 468050 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4819). | ||||
Ref 521763 | ClinicalTrials.gov (NCT00258141) Study With Rupatadine in Mosquito-Bite Allergic Adult Subjects. U.S. National Institutes of Health. | ||||
Ref 521932 | ClinicalTrials.gov (NCT00409305) The Effect of Betahistine on Body Weight in Obese Subjects. U.S. National Institutes of Health. | ||||
Ref 522475 | ClinicalTrials.gov (NCT00784875) An Efficacy Study of Compound LY2624803 in the Treatment of Patients With Chronic Insomnia. U.S. National Institutes of Health. | ||||
Ref 524743 | ClinicalTrials.gov (NCT02132169) A Multi-Center Study Evaluating the Safety of AC-170 0.24%. U.S. National Institutes of Health. | ||||
Ref 527345 | Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children. Br J Clin Pharmacol. 2005 Jan;59(1):43-53. | ||||
Ref 529341 | Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112. | ||||
Ref 534869 | Comparative tolerability of second generation antihistamines. Drug Saf. 1999 May;20(5):385-401. | ||||
Ref 535111 | Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6. | ||||
Ref 535216 | Population pharmacokinetic analysis and optimization of the experimental design for mizolastine solution in children. J Pharmacokinet Pharmacodyn. 2001 Jun;28(3):299-319. | ||||
Ref 535933 | Prescription and safety of dimethindene maleate micropellet capsules in Hungary. Orv Hetil. 2004 Feb 15;145(7):327-9. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 536542 | Desloratadine treatment for intermittent and persistent allergic rhinitis: a review. Clin Ther. 2007 Sep;29(9):1795-802. | ||||
Ref 536700 | Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79. Epub 2008 Apr 29. | ||||
Ref 536923 | Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42. | ||||
Ref 537515 | Antinociception induced by central administration of histamine in the formalin test in rats. Indian J Physiol Pharmacol. 2008 Jul-Sep;52(3):249-54. | ||||
Ref 537884 | Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes. Eur J Pharmacol. 1994 Jan 1;266(1):99-102. | ||||
Ref 538170 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040167. | ||||
Ref 538185 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040519. | ||||
Ref 538228 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070797. | ||||
Ref 538250 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 073283. | ||||
Ref 538351 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083821. | ||||
Ref 538358 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085551. | ||||
Ref 538374 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089013. | ||||
Ref 538375 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089116. | ||||
Ref 538416 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009319. | ||||
Ref 538421 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009495. | ||||
Ref 538458 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012382. | ||||
Ref 538492 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017601. | ||||
Ref 538515 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018746. | ||||
Ref 538587 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022064. | ||||
Ref 538725 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1214). | ||||
Ref 538732 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1220). | ||||
Ref 538734 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1222). | ||||
Ref 538737 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1225). | ||||
Ref 538740 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1228). | ||||
Ref 538761 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1247). | ||||
Ref 538963 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1586). | ||||
Ref 539680 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2603). | ||||
Ref 539685 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2608). | ||||
Ref 541312 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6063). | ||||
Ref 541472 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6326). | ||||
Ref 542007 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6976). | ||||
Ref 542123 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7116). | ||||
Ref 542126 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7119). | ||||
Ref 542129 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7121). | ||||
Ref 542139 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7132). | ||||
Ref 542140 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7133). | ||||
Ref 542141 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7134). | ||||
Ref 542159 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7151). | ||||
Ref 542165 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7157). | ||||
Ref 542174 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7165). | ||||
Ref 542181 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7171). | ||||
Ref 542184 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7174). | ||||
Ref 542186 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7176). | ||||
Ref 542192 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7181). | ||||
Ref 542211 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7199). | ||||
Ref 542220 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7206). | ||||
Ref 542231 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7216). | ||||
Ref 542247 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7231). | ||||
Ref 542253 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7237). | ||||
Ref 542266 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7249). | ||||
Ref 542286 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7267). | ||||
Ref 542302 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7282). | ||||
Ref 542304 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7284). | ||||
Ref 542347 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7324). | ||||
Ref 542352 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7329). | ||||
Ref 542491 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7466). | ||||
Ref 542577 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7587). | ||||
Ref 542578 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7588). | ||||
Ref 544538 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000086) | ||||
Ref 544807 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001178) | ||||
Ref 544859 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001341) | ||||
Ref 545924 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005369) | ||||
Ref 546278 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007218) | ||||
Ref 546280 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007228) | ||||
Ref 547211 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014046) | ||||
Ref 547333 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015252) | ||||
Ref 547977 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020866) | ||||
Ref 548471 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025772) | ||||
Ref 548589 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026836) | ||||
Ref 548731 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028154) | ||||
Ref 525803 | Bioorg Med Chem Lett. 2000 Jun 5;10(11):1277-9.Conformationally-restricted ligands for the histamine H1 receptor. | ||||
Ref 526246 | ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57. | ||||
Ref 526358 | J Pharmacol Exp Ther. 2002 Jul;302(1):328-36.A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors. | ||||
Ref 526569 | Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor. J Pharmacol Exp Ther. 2003 Jun;305(3):1104-15. Epub 2003 Mar 6. | ||||
Ref 527045 | Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species. Nucl Med Biol. 2004 May;31(4):493-502. | ||||
Ref 527113 | Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor. Eur J Biochem. 2004 Jul;271(13):2636-46. | ||||
Ref 527345 | Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children. Br J Clin Pharmacol. 2005 Jan;59(1):43-53. | ||||
Ref 527359 | The effect of a novel, dual function histamine H1 receptor antagonist/5-lipoxygenase enzyme inhibitor on in vivo dermal inflammation and extravasation. Eur J Pharmacol. 2005 Jan 4;506(3):265-71. Epub 2004 Dec 1. | ||||
Ref 527411 | Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5.5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds. | ||||
Ref 527589 | Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21. Epub 2005 Jun 9. | ||||
Ref 527799 | J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm. | ||||
Ref 527929 | Effect of BN 52256 and other mediator antagonists on ouabain-induced cardiac arrhythmia in a model of anaphylaxis in guinea-pigs. Pharmacol Res. 1992 Feb-Mar;25(2):173-80. | ||||
Ref 527955 | Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines. J Pharmacol Exp Ther. 2006 Apr;317(1):139-46. Epub 2006 Jan 4. | ||||
Ref 528242 | A double-blind placebo controlled dose response study of noberastine on histamine induced weal and flare. Eur J Clin Pharmacol. 1991;40(1):83-5. | ||||
Ref 528772 | Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism. | ||||
Ref 529032 | Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. Epub 2007 Sep 10.Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. | ||||
Ref 529341 | Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112. | ||||
Ref 529387 | J Med Chem. 2008 Apr 24;51(8):2457-67. Epub 2008 Mar 22.Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. | ||||
Ref 530299 | Bioorg Med Chem Lett. 2009 Sep 1;19(17):5043-7. Epub 2009 Aug 5.Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs. | ||||
Ref 530300 | J Med Chem. 2009 Sep 10;52(17):5307-10.Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia. | ||||
Ref 530331 | Bioorg Med Chem. 2009 Sep 15;17(18):6496-504. Epub 2009 Aug 13.Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity. | ||||
Ref 530547 | Bioorg Med Chem Lett. 2010 Jan 1;20(1):78-82. Epub 2009 Nov 14.Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. | ||||
Ref 530666 | Bioorg Med Chem. 2010 Feb 15;18(4):1626-32. Epub 2010 Jan 4.Stereoselective synthesis of desloratadine derivatives as antagonist of histamine. | ||||
Ref 531079 | J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. | ||||
Ref 531171 | J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for |A(1)-adrenoceptors. | ||||
Ref 531768 | High-affinity binding of mequitamium iodide (LG 30435) to muscarinic and histamine H1 receptors. Eur J Pharmacol. 1990 Jul 17;182(3):413-20. | ||||
Ref 533039 | Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24(3):401-11. | ||||
Ref 534281 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73. | ||||
Ref 534391 | Studies on the novel antiallergic agent HSR-609: its penetration into the central nervous system in mice and guinea pigs and its selectivity for the histamine H1-receptor. Jpn J Pharmacol. 1997 Apr;73(4):291-8. | ||||
Ref 534845 | Effects of calcium-antagonistic drugs on the stimulation by carbamoylcholine and histamine of phosphatidylinositol turnover in longitudinal smooth muscle of guinea-pig ileum. Biochem J. 1976 Nov 15;160(2):163-9. | ||||
Ref 534867 | A current appreciation of sites for pharmacological intervention in allergic conjunctivitis: effects of new topical ocular drugs. Acta Ophthalmol Scand Suppl. 1999;(228):33-7. | ||||
Ref 534875 | Clinical pharmacology of new histamine H1 receptor antagonists. Clin Pharmacokinet. 1999 May;36(5):329-52. | ||||
Ref 534934 | Combined histamine H1 and H3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion. Am J Rhinol. 1999 Sep-Oct;13(5):391-9. | ||||
Ref 534958 | Histamine as an autocrine regulator of leukemic cell proliferation. Leuk Lymphoma. 2000 Jan;36(3-4):367-73. | ||||
Ref 535111 | Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6. | ||||
Ref 535112 | Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5. | ||||
Ref 535251 | Role of central histaminergic system in lorazepam withdrawal syndrome in rats. Pharmacol Biochem Behav. 2001 Apr;68(4):777-82. | ||||
Ref 535339 | Influence of chronic treatment with H1 receptor antagonists on the anticonvulsant activity of antiepileptic drugs. Pol J Pharmacol. 2001 Jan-Feb;53(1):93-6. | ||||
Ref 535364 | Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7. | ||||
Ref 535368 | Comparison of cyclizine and ondansetron for the prevention of postoperative nausea and vomiting in laparoscopic day-case gynaecological surgery. Anaesthesia. 2002 Jan;57(1):61-5. | ||||
Ref 535477 | Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4. | ||||
Ref 535660 | Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | ||||
Ref 535716 | Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol. Ther Drug Monit. 2003 Apr;25(2):192-6. | ||||
Ref 535805 | Toxicologic and clinical appraisal of buclizine, a new antihistaminic compound. J Allergy. 1956 Jan;27(1):63-7. | ||||
Ref 535848 | Effects of fexofenadine and other antihistamines on components of the allergic response: adhesion molecules. J Allergy Clin Immunol. 2003 Oct;112(4 Suppl):S78-82. | ||||
Ref 535859 | Effects of dimethindene maleate nasal spray on the quality of life in seasonal allergic rhinitis. Rhinology. 2003 Sep;41(3):159-66. | ||||
Ref 535869 | Prostaglandin E2 aggravates gastric mucosal injury induced by histamine in rats through EP1 receptors. Life Sci. 2003 Dec 19;74(5):629-41. | ||||
Ref 535914 | 8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist. Mol Pharmacol. 2004 Mar;65(3):538-49. | ||||
Ref 535933 | Prescription and safety of dimethindene maleate micropellet capsules in Hungary. Orv Hetil. 2004 Feb 15;145(7):327-9. | ||||
Ref 535973 | Influence of antazoline and ketotifen on the anticonvulsant activity of conventional antiepileptics against maximal electroshock in mice. Eur Neuropsychopharmacol. 2004 Aug;14(4):307-18. | ||||
Ref 536000 | Steady-state brain concentrations of antihistamines in rats: interplay of membrane permeability, P-glycoprotein efflux and plasma protein binding. Pharmacology. 2004 Oct;72(2):92-8. | ||||
Ref 536003 | Role of N-methyl-D-aspartate receptors in gastric mucosal blood flow induced by histamine. J Neurosci Res. 2004 Sep 1;77(5):730-8. | ||||
Ref 536086 | Involvement of histamine H1 and H2 receptors in the regulation of STAT-1 phosphorylation: inverse agonism exhibited by the receptor antagonists. Int Immunopharmacol. 2005 Jul;5(7-8):1299-309. | ||||
Ref 536089 | Antihistamines in the treatment of dermatitis. J Cutan Med Surg. 2003 Nov-Dec;7(6):467-73. | ||||
Ref 536153 | Effectiveness of alimemazine in controlling retching after Nissen fundoplication. J Pediatr Surg. 2005 Nov;40(11):1737-40. | ||||
Ref 536284 | Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. | ||||
Ref 536430 | First-generation H1 antihistamines found in pilot fatalities of civil aviation accidents, 1990-2005. Aviat Space Environ Med. 2007 May;78(5):514-22. | ||||
Ref 536469 | Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305. | ||||
Ref 536618 | Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the H1 receptor antagonist clemastine. Arch Pharm Res. 2007 Dec;30(12):1521-5. | ||||
Ref 536700 | Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79. Epub 2008 Apr 29. | ||||
Ref 536707 | The effect of a combined therapy with a histamine H1 antagonist and a chemical mediator release inhibitor on allergic conjunctivitis. Ophthalmologica. 2008;222(4):232-9. Epub 2008 May 8. | ||||
Ref 536717 | Histamine H1-receptor antagonists inhibit nuclear factor-kappaB and activator protein-1 activities via H1-receptor-dependent and -independent mechanisms. Clin Exp Allergy. 2008 Jun;38(6):947-56. | ||||
Ref 536720 | Cyproheptadine displays preclinical activity in myeloma and leukemia. Blood. 2008 Aug 1;112(3):760-9. Epub 2008 May 23. | ||||
Ref 536727 | Small mouse cholangiocytes proliferate in response to H1 histamine receptor stimulation by activation of the IP3/CaMK I/CREB pathway. Am J Physiol Cell Physiol. 2008 Aug;295(2):C499-513. Epub 2008 May 28. | ||||
Ref 536744 | Histamine upregulates keratinocyte MMP-9 production via the histamine H1 receptor. J Invest Dermatol. 2008 Dec;128(12):2783-91. Epub 2008 Jun 12. | ||||
Ref 536767 | Mast cells play a critical role in the pathogenesis of viral myocarditis. Circulation. 2008 Jul 22;118(4):363-72. Epub 2008 Jul 7. | ||||
Ref 536800 | Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62. Epub 2008 Jul 15. | ||||
Ref 536811 | Efficiency of mequitazine in the treatment of allergic rhinitis and chronic urticaria in children. A bibliographic systematic review. Rev Alerg Mex. 2008 Jan-Feb;55(1):3-9. | ||||
Ref 536846 | Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine. Curr Med Chem. 2008;15(21):2173-91. | ||||
Ref 536878 | Histamine 1 receptor antagonist in symptomatic treatment of renal colic accompanied by nausea: two birds with one stone? Urology. 2009 Jan;73(1):32-6. Epub 2008 Oct 11. | ||||
Ref 536896 | Histamine excites rat lateral vestibular nuclear neurons through activation of post-synaptic H2 receptors. Neurosci Lett. 2008 Dec 19;448(1):15-9. Epub 2008 Oct 14. | ||||
Ref 536963 | Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient with the HERG mutation. J Pharmacol Sci. 2008 Dec;108(4):462-71. Epub 2008 Dec 5. | ||||
Ref 537070 | Histamine and the convulsive threshold or effectiveness of antiepileptic drugs. Przegl Lek. 2008;65(11):803-6. | ||||
Ref 537072 | Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8. | ||||
Ref 537098 | Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79. doi: 10.2165/00002018-200932020-00009. | ||||
Ref 537168 | Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors. J Recept Signal Transduct Res. 2009;29(2):84-93. | ||||
Ref 537248 | Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cells in vitro and in vivo. Mediators Inflamm. 2009;2009:738038. Epub 2009 Apr 9. | ||||
Ref 537328 | Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12. Epub 2009 May 14. | ||||
Ref 537347 | Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6. | ||||
Ref 537488 | Design, synthesis and histamine H1-receptor antagonistic activity of some novel 4-amino-2-(substituted)-5-(substituted) aryl-6-[(substituted aryl) amino] pyrimidines. Arzneimittelforschung. 2009;59(5):243-7. | ||||
Ref 537502 | Receptor mediation and nociceptin inhibition of bradykinin-induced plasma extravasation in the knee joint of the rat. Inflamm Res. 2009 Jun 21. | ||||
Ref 537515 | Antinociception induced by central administration of histamine in the formalin test in rats. Indian J Physiol Pharmacol. 2008 Jul-Sep;52(3):249-54. | ||||
Ref 537537 | Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67. | ||||
Ref 537648 | Studies on synergism between penicillins and ambodryl (bromodiphenhydramine HCl), an antihistamine with antimicrobial property. Indian J Exp Biol. 1990 Mar;28(3):253-8. | ||||
Ref 537651 | Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis. Asian Pac J Allergy Immunol. 1990 Dec;8(2):103-7. | ||||
Ref 537703 | Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice. Neuropharmacology. 1985 Jan;24(1):1-4. | ||||
Ref 537714 | The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin. J Allergy Clin Immunol. 1988 Dec;82(6):1113-8. | ||||
Ref 537715 | Identification and differentiation of alkylamine antihistamines and their metabolites in urine by computerized gas chromatography-mass spectrometry. J Chromatogr. 1988 Aug 19;430(1):31-41. | ||||
Ref 537829 | Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain. Naunyn Schmiedebergs Arch Pharmacol. 1994 Feb;349(2):140-4. | ||||
Ref 537846 | The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor. J Med Chem. 1995 Aug 18;38(17):3351-60. | ||||
Ref 537884 | Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes. Eur J Pharmacol. 1994 Jan 1;266(1):99-102. | ||||
Ref 537890 | Synthesis and combined H1-/H2 antagonist activity of mepyramine, pheniramine and cyclizine derivatives with cyanoguanidine, urea and nitroethenediamine partial structures. Arch Pharm (Weinheim). 1994Jul;327(7):455-62. | ||||
Ref 537891 | Transport mechanism of an H1-antagonist at the blood-brain barrier: transport mechanism of mepyramine using the carotid injection technique. Biol Pharm Bull. 1994 May;17(5):676-9. | ||||
Ref 537912 | Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes. J Allergy Clin Immunol. 1994 Mar;93(3):606-14. | ||||
Ref 538066 | Effect of descarboethoxyloratadine, the major metabolite of loratadine, on the human cardiac potassium channel Kv1.5. Br J Pharmacol. 1997 Nov;122(5):796-8. | ||||
Ref 538137 | H2 histaminergic control of inhibition of eating induced by intragastric NaCl in rats. Physiol Behav. 1998 Aug;65(1):105-13. | ||||
Ref 543664 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 262). | ||||
Ref 544069 | Betahistine in the treatment of M?ni?re's disease. Neuropsychiatr Dis Treat. 2007 August; 3(4): 429-440. | ||||
Ref 547978 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020866) | ||||
Ref 551871 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 |
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