Target Information
| Target General Information | Top | |||||
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| Target ID |
T11072
(Former ID: TTDS00100)
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| Target Name |
5-HT 1D receptor (HTR1D)
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| Synonyms |
Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
Click to Show/Hide
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| Gene Name |
HTR1D
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Migraine [ICD-11: 8A80] | |||||
| 2 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
| Function |
Functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN EEFRQAFQKIVPFRKAS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 5 Approved Drugs | + | ||||
| 1 | Almogran | Drug Info | Approved | Migraine | [5] | |
| 2 | Eletriptan | Drug Info | Approved | Migraine | [3], [6] | |
| 3 | Frovatriptan | Drug Info | Approved | Migraine | [3], [7] | |
| 4 | Rizatriptan | Drug Info | Approved | Migraine | [8] | |
| 5 | Zolmitriptan | Drug Info | Approved | Migraine | [9], [10] | |
| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | Neu-P11 | Drug Info | Phase 2 | Insomnia | [11] | |
| 2 | NXN-188 | Drug Info | Phase 2 | Migraine | [12] | |
| 3 | TGBA01AD | Drug Info | Phase 2 | Mood disorder | [13] | |
| 4 | Tonabersat | Drug Info | Phase 2 | Epilepsy | [14] | |
| Discontinued Drug(s) | [+] 12 Discontinued Drugs | + | ||||
| 1 | Avitriptan | Drug Info | Discontinued in Phase 3 | Migraine | [17] | |
| 2 | BMS-181101 | Drug Info | Discontinued in Phase 2 | Mood disorder | [18], [19] | |
| 3 | CP-122288 | Drug Info | Discontinued in Phase 2 | Migraine | [20], [21] | |
| 4 | Elzasonan hydrochloride | Drug Info | Discontinued in Phase 2 | Mood disorder | [13] | |
| 5 | IS-159 | Drug Info | Discontinued in Phase 2 | Migraine | [22] | |
| 6 | PNU-142633 | Drug Info | Discontinued in Phase 2 | Migraine | [23] | |
| 7 | ALX-0646 | Drug Info | Discontinued in Phase 1 | Migraine | [24] | |
| 8 | Tidembersat | Drug Info | Discontinued in Phase 1 | Migraine | [25] | |
| 9 | BMS-181885 | Drug Info | Terminated | Migraine | [29] | |
| 10 | GR-127935 | Drug Info | Terminated | Major depressive disorder | [30], [31] | |
| 11 | L-694247 | Drug Info | Terminated | Migraine | [32], [33] | |
| 12 | PNU-109291 | Drug Info | Terminated | Migraine | [34], [35] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | Donitriptan | Drug Info | Preclinical | Migraine | [26], [27] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Agonist | [+] 29 Agonist drugs | + | ||||
| 1 | Almogran | Drug Info | [36] | |||
| 2 | Rizatriptan | Drug Info | [38] | |||
| 3 | FKB01MD | Drug Info | [39] | |||
| 4 | Neu-P11 | Drug Info | [40] | |||
| 5 | Tonabersat | Drug Info | [43], [44] | |||
| 6 | Avitriptan | Drug Info | [44], [45] | |||
| 7 | CP-122288 | Drug Info | [44], [47] | |||
| 8 | PNU-142633 | Drug Info | [44], [50] | |||
| 9 | ALX-0646 | Drug Info | [44] | |||
| 10 | BMS-181885 | Drug Info | [44], [46] | |||
| 11 | L-694247 | Drug Info | [44], [53] | |||
| 12 | PNU-109291 | Drug Info | [44], [56] | |||
| 13 | 1-naphthylpiperazine | Drug Info | [59], [65] | |||
| 14 | 2-methyl-5-HT | Drug Info | [69] | |||
| 15 | 5-CT | Drug Info | [71] | |||
| 16 | 7-methoxy-1-naphthylpiperazine | Drug Info | [64] | |||
| 17 | alpha-methyl-5-HT | Drug Info | [69] | |||
| 18 | BRL-15572 | Drug Info | [74] | |||
| 19 | dipropyl-5-CT | Drug Info | [65] | |||
| 20 | EDMT | Drug Info | [75] | |||
| 21 | lysergic acid | Drug Info | [69] | |||
| 22 | lysergol | Drug Info | [65] | |||
| 23 | SB 216641 | Drug Info | [74] | |||
| 24 | [125I]GTI | Drug Info | [81] | |||
| 25 | [3H]5-CT | Drug Info | [82] | |||
| 26 | [3H]5-HT | Drug Info | [83] | |||
| 27 | [3H]8-OH-DPAT | Drug Info | [84] | |||
| 28 | [3H]eletriptan | Drug Info | [85] | |||
| 29 | [3H]sumatriptan | Drug Info | [85] | |||
| Modulator | [+] 9 Modulator drugs | + | ||||
| 1 | Eletriptan | Drug Info | [37] | |||
| 2 | Frovatriptan | Drug Info | [37] | |||
| 3 | Zolmitriptan | Drug Info | [37] | |||
| 4 | NXN-188 | Drug Info | [41] | |||
| 5 | TGBA01AD | Drug Info | [42] | |||
| 6 | Elzasonan hydrochloride | Drug Info | [48] | |||
| 7 | IS-159 | Drug Info | [49] | |||
| 8 | Donitriptan | Drug Info | [51] | |||
| 9 | GR-127935 | Drug Info | [52] | |||
| Antagonist | [+] 10 Antagonist drugs | + | ||||
| 1 | BMS-181101 | Drug Info | [44], [46] | |||
| 2 | Tidembersat | Drug Info | [44] | |||
| 3 | bufotenine | Drug Info | [69] | |||
| 4 | L-772,405 | Drug Info | [77] | |||
| 5 | m-chlorophenylpiperazine | Drug Info | [71] | |||
| 6 | MPDT | Drug Info | [75] | |||
| 7 | SB 272183 | Drug Info | [78] | |||
| 8 | SB 649915 | Drug Info | [79] | |||
| 9 | SB 714786 | Drug Info | [79] | |||
| 10 | [3H]GR 125,743 | Drug Info | [82] | |||
| Inhibitor | [+] 45 Inhibitor drugs | + | ||||
| 1 | L-741604 | Drug Info | [54] | |||
| 2 | L-775606 | Drug Info | [55] | |||
| 3 | (+/-)-nantenine | Drug Info | [57] | |||
| 4 | (3-Chloro-phenyl)-piperazin-1-yl-methanone | Drug Info | [58] | |||
| 5 | 1,2,3,4-Tetrahydro-naphthalen-2-ylamine | Drug Info | [59] | |||
| 6 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [60] | |||
| 7 | 1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine | Drug Info | [58] | |||
| 8 | 1-(2,5-Dimethoxy-phenyl)-piperazine | Drug Info | [58] | |||
| 9 | 1-(2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [61] | |||
| 10 | 1-(2-Butoxy-phenyl)-piperazine | Drug Info | [62] | |||
| 11 | 1-(2-Ethoxy-phenyl)-piperazine | Drug Info | [62] | |||
| 12 | 1-(2-Fluoro-phenyl)-piperazine | Drug Info | [62] | |||
| 13 | 1-(2-Isopropoxy-phenyl)-piperazine | Drug Info | [62] | |||
| 14 | 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [63] | |||
| 15 | 1-(3-Fluoro-phenyl)-piperazine | Drug Info | [62] | |||
| 16 | 1-(3-Nitro-phenyl)-piperazine | Drug Info | [62] | |||
| 17 | 1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine | Drug Info | [58] | |||
| 18 | 1-(7-Methoxy-naphthalen-2-yl)-piperazine | Drug Info | [64] | |||
| 19 | 2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole | Drug Info | [66] | |||
| 20 | 2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol | Drug Info | [61] | |||
| 21 | 2-(2-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [61] | |||
| 22 | 2-(3-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [61] | |||
| 23 | 2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [61] | |||
| 24 | 2-(4-Bromo-phenyl)-1-methyl-ethylamine | Drug Info | [61] | |||
| 25 | 2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole | Drug Info | [66] | |||
| 26 | 2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine | Drug Info | [67] | |||
| 27 | 2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine | Drug Info | [68] | |||
| 28 | 2-Piperazin-1-yl-benzonitrile | Drug Info | [62] | |||
| 29 | 2-Piperazin-1-yl-phenol | Drug Info | [58] | |||
| 30 | 3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one | Drug Info | [58] | |||
| 31 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [70] | |||
| 32 | 5-amino-3-(N-methylpiperidin-4-yl)-1H-indole | Drug Info | [55] | |||
| 33 | 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [70] | |||
| 34 | 5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole | Drug Info | [72] | |||
| 35 | 5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole | Drug Info | [72] | |||
| 36 | 8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline | Drug Info | [59] | |||
| 37 | 8-Methoxy-2-piperazin-1-yl-quinoline | Drug Info | [59] | |||
| 38 | 8-Methoxy-quinolin-2-ylamine | Drug Info | [59] | |||
| 39 | AGROCLAVINE | Drug Info | [73] | |||
| 40 | Brolamfetamine | Drug Info | [61] | |||
| 41 | L-747201 | Drug Info | [76] | |||
| 42 | QUIPAZINE | Drug Info | [59] | |||
| 43 | SEROTONIN | Drug Info | [55] | |||
| 44 | WAY-466 | Drug Info | [80] | |||
| 45 | [2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine | Drug Info | [72] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Pathway Affiliation
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| cAMP signaling pathway | hsa04024 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Serotonergic synapse | hsa04726 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Taste transduction | hsa04742 | Affiliated Target |
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| Class: Organismal Systems => Sensory system | Pathway Hierarchy | ||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | cAMP signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Serotonergic synapse | |||||
| Panther Pathway | [+] 2 Panther Pathways | + | ||||
| 1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
| 2 | 5HT1 type receptor mediated signaling pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Serotonin receptors | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Serotonin HTR1 Group and FOS Pathway | |||||
| 2 | Monoamine GPCRs | |||||
| 3 | GPCRs, Class A Rhodopsin-like | |||||
| 4 | GPCR ligand binding | |||||
| 5 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32. | |||||
| REF 2 | URL: 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: 54). | |||||
| REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | Drug information of Almogran, 2008. eduDrugs. | |||||
| REF 6 | URL: 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: 40). | |||||
| REF 7 | URL: 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: 7191). | |||||
| REF 8 | Clinical pipeline report, company report or official report of Intelgenx. | |||||
| REF 9 | URL: 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: 60). | |||||
| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020768. | |||||
| REF 11 | ClinicalTrials.gov (NCT01489969) Sleep Laboratory Study to Investigate the Safety and Efficacy of Neu-P11 in Primary Insomnia Patients. U.S. National Institutes of Health. | |||||
| REF 12 | ClinicalTrials.gov (NCT00920686) Study of NXN 188 for the Treatment of Migraine With Aura. U.S. National Institutes of Health. | |||||
| REF 13 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
| REF 14 | ClinicalTrials.gov (NCT00534560) Dose Ranging Study of the Efficacy and Tolerability of Tonabersat in the Prophylaxis of Migraine Headache. U.S. National Institutes of Health. | |||||
| REF 15 | URL: 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: 120). | |||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006286) | |||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002927) | |||||
| REF 18 | URL: 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: 108). | |||||
| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005177) | |||||
| REF 20 | URL: 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: 110). | |||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005787) | |||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005786) | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013927) | |||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008400) | |||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010348) | |||||
| REF 26 | URL: 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: 39). | |||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012002) | |||||
| REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023937) | |||||
| REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007062) | |||||
| REF 30 | URL: 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: 14). | |||||
| REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002743) | |||||
| REF 32 | URL: 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: 15). | |||||
| REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003457) | |||||
| REF 34 | URL: 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: 3228). | |||||
| REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010481) | |||||
| REF 36 | Efficacy and tolerability of subcutaneous almotriptan for the treatment of acute migraine: a randomized, double-blind, parallel-group, dose-finding study. Clin Ther. 2001 Nov;23(11):1867-75. | |||||
| REF 37 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 38 | An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. | |||||
| REF 39 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 40 | Clinical pipeline report, company report or official report of Neurim Pharmaceuticals. | |||||
| REF 41 | Company report (NeurAxon) | |||||
| REF 42 | Company report (Fabrekramer) | |||||
| REF 43 | The potential anti-migraine compound SB-220453 does not contract human isolated blood vessels or myocardium; a comparison with sumatriptan. Cephalalgia. 2000 Jul;20(6):538-45. | |||||
| REF 44 | Sustained pain relief with dihydroergotamine in migraine is potentially due to persistent binding to 5-HT1B and 5-HT1D receptors. . The Journal of Headache and Pain 201314(Suppl 1):P75. | |||||
| REF 45 | Safety trial with the 5HT1B/1D agonist avitriptan (BMS-180048) in patients with migraine who have experienced pressure, tightness, and/or pain in the chest, neck, and/or throat following sumatriptan.Cephalalgia. 1998 Oct;18(8):546-51. | |||||
| REF 46 | Sensitive triple-quadrupole mass spectrometric assay for the determination of BMS-181885, a 5-HT1 agonist, in human plasma following solid phase extraction. Biomed Chromatogr. 1999 Oct;13(6):425-30. | |||||
| REF 47 | The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater. Neuropharmacology. 1997 Jan;36(1):83-91. | |||||
| REF 48 | DOI: 10.1002/9781118541203.xen439 | |||||
| REF 49 | Pronounced effect of caprylocaproyl macrogolglycerides on nasal absorption of IS-159, a peptide serotonin 1B/1D-receptor agonist. Clin Pharmacol Ther. 2000 Aug;68(2):114-21. | |||||
| REF 50 | Further characterization of the 5-HT1 receptors mediating cardiac sympatho-inhibition in pithed rats: pharmacological correlation with the 5-HT1B a... Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):220-7. | |||||
| REF 51 | Donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors.Br J Pharmacol.2006 Sep;149(1):82-91. | |||||
| REF 52 | GR127935: a potent and selective 5-HT1D receptor antagonist.Behav Brain Res.1996;73(1-2):157-61. | |||||
| REF 53 | L-694,247: a potent 5-HT1D receptor agonist. Br J Pharmacol. 1993 Nov;110(3):1196-200. | |||||
| REF 54 | 3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1999 Feb 25;42(4):691-705. | |||||
| REF 55 | Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-pip... J Med Chem. 2008 Jun 26;51(12):3609-16. | |||||
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