Target Information

Target General Infomation
Target ID
T87023
Former ID
TTDR01165
Target Name
Platelet-activating factor receptor
Gene Name
PTAFR
Synonyms
PAF-R; PTAFR
Target Type
Successful
Disease Asthma [ICD10: J45]
Allergy [ICD9: 995.3; ICD10: T78.4]
Brain ischaemia [ICD9: 435, 437; ICD10: G45.9, I67.8]
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49]
Conjunctivitis [ICD9: 372; ICD10: H10]
Cerebral infarction [ICD10: I63]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Nerve injury [ICD10: T14.4]
Ocular allergy [ICD9: 360-379; ICD10: H00-H59]
Psoriasis [ICD9: 696; ICD10: L40]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Stroke [ICD9: 434.91, 437.6, 453, 671.5, 671.9; ICD10: I61-I63, I80-I82]
Septic shock [ICD9: 785.52; ICD10: A41.9]
Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Thrombocytopenia [ICD9: 287.3, 287.4, 287.5; ICD10: D69.6, P61.0]
Unspecified [ICD code not available]
Function
Receptor for platelet activating factor, a chemotactic phospholipid mediator that possesses potent inflammatory, smooth- muscle contractile and hypotensive activity. Seems to mediate its action via a G protein that activates a phosphatidylinositol- calcium second messenger system.
BioChemical Class
GPCR rhodopsin
Target Validation
T87023
UniProt ID
P25105
Sequence
MEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLT
MADMLFLITLPLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVT
RPIKTAQANTRKRGISLSLVIWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKG
SVPVLIIHIFIVFSFFLVFLIILFCNLVIIRTLLMQPVQQQRNAEVKRRALWMVCTVLAV
FIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLCLLSTNCVLDPVIYCFLTKKF
RKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN
Drugs and Mode of Action
Drug(s) Ticlopidine Drug Info Approved Stroke [536186], [542329]
RUPATADINE Drug Info Phase 4 Discovery agent [521763]
ISRAPAFANT Drug Info Phase 3 Asthma [539166], [544953]
CMI-392 Drug Info Phase 2 Psoriasis [526130]
Dersalazine Drug Info Phase 2 Inflammatory bowel disease [544223]
Lexipafant Drug Info Phase 2 Nerve injury [533596]
YM-264 Drug Info Phase 2 Septic shock [551827]
BN 50730 Drug Info Discontinued in Phase 3 Asthma [544860]
FOROPAFANT Drug Info Discontinued in Phase 3 Asthma [539165], [545088]
BN50727 Drug Info Discontinued in Phase 2 Inflammatory bowel disease [545900]
DE-081 Drug Info Discontinued in Phase 2 Conjunctivitis [544551]
E-6123 Drug Info Discontinued in Phase 2 Asthma [544861]
Minopafant Drug Info Discontinued in Phase 2 Septic shock [545101]
MK-287 Drug Info Discontinued in Phase 2 Septic shock [544956]
Ro-24-4736 Drug Info Discontinued in Phase 2 Septic shock [544808]
SM-10661 Drug Info Discontinued in Phase 2 Septic shock [545724]
TCV-309 Drug Info Discontinued in Phase 2 Septic shock [545100]
UK-74505 Drug Info Discontinued in Phase 2 Septic shock [544958]
ABT-299 Drug Info Discontinued in Phase 1 Septic shock [539158], [545958]
AGN-191743 Drug Info Discontinued in Phase 1 Allergy [545538]
DACOPAFANT Drug Info Discontinued in Phase 1 Septic shock [544523]
DF-1111301 Drug Info Discontinued in Phase 1 Allergy [545558]
SDZ-62-434 Drug Info Discontinued in Phase 1 Solid tumours [545067]
Apafant Drug Info Terminated Ocular allergy [536119], [539170]
Bepafant Drug Info Terminated Septic shock [541324], [544548]
BN-50726 Drug Info Terminated Nerve injury [544993]
BN50739 Drug Info Terminated Cerebral infarction [539160], [545069]
BN52021 Drug Info Terminated Septic shock [539172], [544554]
CL-184005 Drug Info Terminated Septic shock [544950]
CMI-206 Drug Info Terminated Inflammatory disease [551572]
CV 6209 Drug Info Terminated Asthma [539161], [544844]
FR-128998 Drug Info Terminated Thrombocytopenia [545711]
KC-11404 Drug Info Terminated Asthma [533776]
KC-11425 Drug Info Terminated Asthma [545947]
L-659989 Drug Info Terminated Discovery agent [540368], [545703]
Ro-24-0238 Drug Info Terminated Septic shock [545571]
SCH-37370 Drug Info Terminated Discovery agent [544522]
Sch-40338 Drug Info Terminated Allergy [529095], [539163]
SDZ-64-412 Drug Info Terminated Discovery agent [539164], [544521]
TIAPAFANT Drug Info Terminated Septic shock [541326], [545057]
TULOPAFANT Drug Info Terminated Cardiac arrhythmias [544829]
UR-12460 Drug Info Terminated Thromboembolism [545849]
WEB-2347 Drug Info Terminated Allergy [544959]
Antagonist 10-OBn-7alpha-F-gingkolide B Drug Info [526536]
10-OBn-epi-ginkgolide C Drug Info [526536]
10-OBn-ginkgolide B Drug Info [526536]
10-OBn-ginkgolide C Drug Info [526536]
7-epi-ginkgolide C Drug Info [526536]
7alpha-Cl-ginkgolide B Drug Info [526536]
7alpha-F-ginkgolide B Drug Info [526536]
7alpha-N3-ginkgolide B Drug Info [526536]
7alpha-NH2-ginkgolide B Drug Info [526536]
7alpha-NHEt-ginkgolide B Drug Info [526536]
7alpha-NHMe-ginkgolide B Drug Info [526536]
7alpha-OAc-ginkgolide B Drug Info [526536]
7alpha-OCOCH2Ph-ginkgolide B Drug Info [526536]
ABT-299 Drug Info [534237]
Apafant Drug Info [536119]
Bepafant Drug Info [531921]
BN-50726 Drug Info [526932]
CV-3988 Drug Info [533398]
DACOPAFANT Drug Info [531635], [532945]
DF-1111301 Drug Info [531635], [550948]
FOROPAFANT Drug Info [525756], [528090], [531635]
ISRAPAFANT Drug Info [530579], [531635]
KC-11425 Drug Info [551926]
LAU-0901 Drug Info [529694], [531839]
Minopafant Drug Info [527485]
MK-287 Drug Info [531635], [534027]
Ro-24-4736 Drug Info [528091]
RP-52770 Drug Info [533359]
SDZ-62-434 Drug Info [531635], [534010]
SM-10661 Drug Info [531635], [534276]
TIAPAFANT Drug Info [531635], [533646]
TULOPAFANT Drug Info [531635], [534023]
UK-74505 Drug Info [533761]
YM-264 Drug Info [530793]
[3H]52770 RP Drug Info [533359]
[3H]apafant Drug Info [533649]
Agonist 2-O-ethyl-PAF C-16 Drug Info [533649]
2-O-methyl-PAF C-18 Drug Info [533649]
enantio PAF C-16 Drug Info [533649]
methylcarbamyl PAF Drug Info [543773]
PAF Drug Info [534204]
[3H]PAF Drug Info [526143]
Modulator A 137491 Drug Info [538075]
AGN-191743 Drug Info [550918]
BB-823 Drug Info [533626]
BN 50730 Drug Info
BN50727 Drug Info
BN50739 Drug Info
BN52021 Drug Info
CL-184005 Drug Info
CMI-206 Drug Info
CMI-392 Drug Info [526130]
CV 6209 Drug Info
DE-081 Drug Info [534251]
E-6123 Drug Info
FR-128998 Drug Info [533881]
FR-900452 Drug Info
KC-11404 Drug Info [533776]
KO-286011 Drug Info
Lexipafant Drug Info
SCH-37370 Drug Info [529095]
Sch-40338 Drug Info
SRI-63-675 Drug Info
TCV-309 Drug Info
Ticlopidine Drug Info [556264]
UR-10324 Drug Info
UR-11353 Drug Info
UR-12460 Drug Info [533626]
UR-12510 Drug Info [550919]
UR-12519 Drug Info
WEB-2347 Drug Info [529756]
Inhibitor Dersalazine Drug Info [544223]
L-652731 Drug Info [526814]
L-659989 Drug Info [526814]
Platelet activating factor receptor inhibitors Drug Info [543773]
Ro-24-0238 Drug Info [533343]
RUPATADINE Drug Info [527799]
SDZ-64-412 Drug Info [533935]
VERAGUENSIN Drug Info [526814]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Staphylococcus aureus infection
NetPath Pathway IL5 Signaling Pathway
Leptin Signaling Pathway
Reactome Class A/1 (Rhodopsin-like receptors)
G alpha (q) signalling events
Interferon gamma signaling
WikiPathways GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Small Ligand GPCRs
Interferon gamma signaling
GPCR ligand binding
GPCR downstream signaling
References
Ref 521763ClinicalTrials.gov (NCT00258141) Study With Rupatadine in Mosquito-Bite Allergic Adult Subjects. U.S. National Institutes of Health.
Ref 526130Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20.
Ref 529095Sch 37370: a new drug combining antagonism of platelet-activating factor (PAF) with antagonism of histamine. Agents Actions Suppl. 1991;34:313-21.
Ref 533596Randomized, double-blind phase II trial of Lexipafant, a platelet-activating factor antagonist, in human acute pancreatitis. Br J Surg. 1995 Oct;82(10):1414-20.
Ref 533776Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995 Feb 17;38(4):669-85.
Ref 536119Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
Ref 536186Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
Ref 539158(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: 1849).
Ref 539160(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: 1851).
Ref 539161(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: 1852).
Ref 539163(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: 1854).
Ref 539164(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: 1855).
Ref 539165(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: 1856).
Ref 539166(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: 1857).
Ref 539170(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: 1860).
Ref 539172(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: 1862).
Ref 540368(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: 3426).
Ref 541324(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: 6078).
Ref 541326(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: 6080).
Ref 542329(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: 7307).
Ref 544223The intestinal anti-inflammatory effect of dersalazine sodium is related to a down-regulation in IL-17 production in experimental models of rodent colitis. Br J Pharmacol. 2012 February; 165(3): 729-740.
Ref 544521Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000046)
Ref 544522Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000047)
Ref 544523Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000051)
Ref 544548Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000108)
Ref 544551Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000113)
Ref 544554Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000117)
Ref 544808Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001180)
Ref 544829Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001254)
Ref 544844Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001311)
Ref 544860Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001346)
Ref 544861Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001351)
Ref 544950Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001674)
Ref 544953Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001699)
Ref 544956Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001713)
Ref 544958Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001719)
Ref 544959Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001720)
Ref 544993Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001821)
Ref 545057Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001989)
Ref 545067Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002021)
Ref 545069Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002032)
Ref 545088Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002078)
Ref 545100Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002130)
Ref 545101Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002131)
Ref 545538Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003636)
Ref 545558Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003701)
Ref 545571Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003729)
Ref 545703Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004265)
Ref 545711Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004313)
Ref 545724Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004382)
Ref 545849Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005037)
Ref 545900Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005290)
Ref 545947Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005461)
Ref 545958Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005514)
Ref 551572Cmi206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor. Bioorganic & Medicinal Chemistry Letters. 03/1995; 5(6):643-648.
Ref 551827Current Pharmaceutical Design. Page(175).
Ref 525756In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist, on the PAF-induced bovine platelet aggregation. Vet Res. 2000 Mar-Apr;31(2):267-72.
Ref 526130Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20.
Ref 526143Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation. J Biol Chem. 2001 Nov 16;276(46):43025-30. Epub 2001 Sep 17.
Ref 526536Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists. J Med Chem. 2003 Feb 13;46(4):601-8.
Ref 526814J Med Chem. 1992 Sep 18;35(19):3474-82.Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.
Ref 526932Effects of the PAF antagonists BN50726 and BN50739 on arrhythmogenesis and extent of necrosis during myocardial ischaemia/reperfusion in rabbits. Br J Pharmacol. 1992 Nov;107(3):705-9.
Ref 527485Formation of spherical micelles composed of the novel platelet activating factor receptor antagonist, E5880. Pharm Dev Technol. 2005;10(1):11-6.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 528090Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist. J Pharmacol Exp Ther. 1991 Oct;259(1):44-51.
Ref 528091Pharmacology of a potent platelet-activating factor antagonist: Ro 24-4736. J Pharmacol Exp Ther. 1991 Oct;259(1):78-85.
Ref 529095Sch 37370: a new drug combining antagonism of platelet-activating factor (PAF) with antagonism of histamine. Agents Actions Suppl. 1991;34:313-21.
Ref 529694LAU-0901, a novel platelet-activating factor antagonist, is highly neuroprotective in cerebral ischemia. Exp Neurol. 2008 Dec;214(2):253-8.
Ref 529756WEB 2347: pharmacology of a new very potent and long acting hetrazepinoic PAF-antagonist and its action in repeatedly sensitized guinea-pigs. J Lipid Mediat. 1991 Jul-Aug;4(1):39-44.
Ref 530579Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor. J Biol Chem. 2010 Feb 19;285(8):5931-40.
Ref 530793Effects of YM264, a novel PAF antagonist, on puromycin aminonucleoside-induced nephropathy in the rat. Biochem Biophys Res Commun. 1991 Apr 30;176(2):781-5.
Ref 531635Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
Ref 531839Superior Neuroprotective Efficacy of LAU-0901, a Novel Platelet-Activating Factor Antagonist, in Experimental Stroke. Transl Stroke Res. 2012 Mar;3(1):154-63.
Ref 531921Pharmacologic activity of bepafant (WEB 2170), a new and selective hetrazepinoic antagonist of platelet activating factor. J Pharmacol Exp Ther. 1990 Dec;255(3):962-8.
Ref 532945RP 55778, a PAF receptor antagonist, prevents and reverses LPS-induced hemoconcentration and TNF release. J Lipid Mediat. 1989 Nov-Dec;1(6):349-60.
Ref 533343J Med Chem. 1989 Aug;32(8):1820-35.Pentadienyl carboxamide derivatives as antagonists of platelet-activating factor.
Ref 533359[3H]52770 RP, a platelet-activating factor receptor antagonist, and tritiated platelet-activating factor label a common specific binding site in human polymorphonuclear leukocytes. J Pharmacol Exp Ther. 1988 Feb;244(2):709-15.
Ref 533398Inhibition by CV-3988 of the binding of [3H]-platelet activating factor (PAF) to the platelet. Biochem Pharmacol. 1985 May 1;34(9):1491-5.
Ref 533626Platelet-activating factor: the effector of protein-rich plasma extravasation and nitric oxide synthase induction in rat immune complex peritonitis. Br J Pharmacol. 1995 Feb;114(4):895-901.
Ref 533646PCA-4248, a PAF receptor antagonist, inhibits PAF-induced phosphoinositide turnover. Eur J Pharmacol. 1995 Aug 15;290(3):183-8.
Ref 533649A radioreceptor binding assay for platelet-activating factor (PAF) using membranes from CHO cells expressing human PAF receptor. J Immunol Methods. 1995 Oct 26;186(2):225-31.
Ref 533761Differential effects of the PAF receptor antagonist UK-74,505 on neutrophil and eosinophil accumulation in guinea-pig skin. Br J Pharmacol. 1994 Oct;113(2):513-21.
Ref 533776Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995 Feb 17;38(4):669-85.
Ref 533881Effect of FR128998, a novel PAF receptor antagonist, on endotoxin-induced disseminated intravascular coagulation. Eur J Pharmacol. 1994 Jun 13;258(3):239-46.
Ref 533935J Med Chem. 1993 Oct 15;36(21):3098-102.Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists.
Ref 534010In vitro antitumour activity of the novel imidazoisoquinoline SDZ 62-434. Br J Cancer. 1993 May;67(5):989-95.
Ref 534023Tulopafant, a PAF receptor antagonist, increases capillary patency and prolongs survival in discordant cardiac xenotransplants. J Lipid Mediat. 1993 May;7(1):79-84.
Ref 534027MK 287: a potent, specific, and orally active receptor antagonist of platelet-activating factor. J Lipid Mediat. 1993 Jun;7(2):115-34.
Ref 534204Identification of transmembrane domain residues determinant in the structure-function relationship of the human platelet-activating factor receptor by site-directed mutagenesis. J Biol Chem. 1996 Sep20;271(38):23298-303.
Ref 534237ABT-299, a novel PAF antagonist, attenuates multiple effects of endotoxemia in conscious rats. Shock. 1996 Aug;6(2):112-7.
Ref 534251J Pharmacol Toxicol Methods. 1996 Sep;36(1):53-62.Characterization of [3H]apafant binding to PAF receptor on rabbit platelet membranes: a comparison of a microplate filtration system and a standard method.
Ref 534276Effect of the PAF-receptor antagonist SM-12502 on human platelets. Inflammation. 1996 Feb;20(1):71-85.
Ref 536119Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
Ref 538075The role of platelet-activating factor (PAF) and the efficacy of ABT-491, a highly potent and selective PAF antagonist, in experimental allergic rhinitis. J Pharmacol Exp Ther. 1998 Jan;284(1):83-8.
Ref 543773(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: 334).
Ref 544223The intestinal anti-inflammatory effect of dersalazine sodium is related to a down-regulation in IL-17 production in experimental models of rodent colitis. Br J Pharmacol. 2012 February; 165(3): 729-740.
Ref 550918US patent application no. 6,274,627, Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor.
Ref 550919US patent application no. 6,673,908, Tumor necrosis factor receptor 2.
Ref 550948US patent application no. 2007,0196,421, Soft tissue implants and drug combination compositions, and use thereof.
Ref 551926WO patent application no. 2002,01223,5, 1,4-dihydropyridines as bradykinin antagonists.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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