Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T11072
(Former ID: TTDS00100)
|
|||||
Target Name |
5-HT 1D receptor (HTR1D)
|
|||||
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
|
|||||
Gene Name |
HTR1D
|
|||||
Target Type |
Successful target
|
[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
|
|||||
BioChemical Class |
GPCR rhodopsin
|
|||||
UniProt ID | ||||||
Sequence |
MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN EEFRQAFQKIVPFRKAS Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Approved Drug(s) | [+] 7 Approved Drugs | + | ||||
1 | Almogran | Drug Info | Approved | Migraine | [2] | |
2 | Eletriptan | Drug Info | Approved | Migraine | [3], [4] | |
3 | Frovatriptan | Drug Info | Approved | Migraine | [4], [5] | |
4 | Metergolin | Drug Info | Approved | Hyperprolactinaemia | [6] | |
5 | Rizatriptan | Drug Info | Approved | Migraine | [7] | |
6 | Sumatriptan | Drug Info | Approved | Migraine | [4], [8] | |
7 | 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) | [+] 14 Discontinued Drugs | + | ||||
1 | Alniditan | Drug Info | Discontinued in Phase 3 | Migraine | [15], [16] | |
2 | Avitriptan | Drug Info | Discontinued in Phase 3 | Migraine | [17] | |
3 | BMS-181101 | Drug Info | Discontinued in Phase 2 | Mood disorder | [18], [19] | |
4 | CP-122288 | Drug Info | Discontinued in Phase 2 | Migraine | [20], [21] | |
5 | Elzasonan hydrochloride | Drug Info | Discontinued in Phase 2 | Mood disorder | [13] | |
6 | IS-159 | Drug Info | Discontinued in Phase 2 | Migraine | [22] | |
7 | PNU-142633 | Drug Info | Discontinued in Phase 2 | Migraine | [23] | |
8 | ALX-0646 | Drug Info | Discontinued in Phase 1 | Migraine | [24] | |
9 | Tidembersat | Drug Info | Discontinued in Phase 1 | Migraine | [25] | |
10 | BMS-181885 | Drug Info | Terminated | Migraine | [28] | |
11 | GR-127935 | Drug Info | Terminated | Major depressive disorder | [29], [30] | |
12 | L-694247 | Drug Info | Terminated | Migraine | [31], [32] | |
13 | PNU-109291 | Drug Info | Terminated | Migraine | [33], [34] | |
14 | VR-147 | Drug Info | Terminated | Migraine | [35] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | Donitriptan | Drug Info | Preclinical | Migraine | [26], [27] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Agonist | [+] 32 Agonist drugs | + | ||||
1 | Almogran | Drug Info | [36] | |||
2 | Rizatriptan | Drug Info | [39] | |||
3 | Sumatriptan | Drug Info | [1], [40], [41], [42], [43] | |||
4 | FKB01MD | Drug Info | [44] | |||
5 | Neu-P11 | Drug Info | [45] | |||
6 | Tonabersat | Drug Info | [48], [49] | |||
7 | Alniditan | Drug Info | [50], [49], [50] | |||
8 | Avitriptan | Drug Info | [51], [49] | |||
9 | CP-122288 | Drug Info | [53], [49] | |||
10 | PNU-142633 | Drug Info | [56], [49] | |||
11 | ALX-0646 | Drug Info | [49] | |||
12 | BMS-181885 | Drug Info | [52], [49] | |||
13 | L-694247 | Drug Info | [59], [49] | |||
14 | PNU-109291 | Drug Info | [62], [49] | |||
15 | 1-naphthylpiperazine | Drug Info | [72], [66] | |||
16 | 2-methyl-5-HT | Drug Info | [76] | |||
17 | 5-CT | Drug Info | [38] | |||
18 | 7-methoxy-1-naphthylpiperazine | Drug Info | [71] | |||
19 | alpha-methyl-5-HT | Drug Info | [76] | |||
20 | BRL-15572 | Drug Info | [81] | |||
21 | dipropyl-5-CT | Drug Info | [72] | |||
22 | EDMT | Drug Info | [82] | |||
23 | lysergic acid | Drug Info | [76] | |||
24 | lysergol | Drug Info | [72] | |||
25 | SB 216641 | Drug Info | [81] | |||
26 | TFMPP | Drug Info | [38], [65] | |||
27 | [125I]GTI | Drug Info | [89] | |||
28 | [3H]5-CT | Drug Info | [90] | |||
29 | [3H]5-HT | Drug Info | [50] | |||
30 | [3H]8-OH-DPAT | Drug Info | [91] | |||
31 | [3H]eletriptan | Drug Info | [92] | |||
32 | [3H]sumatriptan | Drug Info | [92] | |||
Modulator | [+] 10 Modulator drugs | + | ||||
1 | Eletriptan | Drug Info | [37] | |||
2 | Frovatriptan | Drug Info | [37] | |||
3 | Zolmitriptan | Drug Info | [37] | |||
4 | NXN-188 | Drug Info | [46] | |||
5 | TGBA01AD | Drug Info | [47] | |||
6 | Elzasonan hydrochloride | Drug Info | [54] | |||
7 | IS-159 | Drug Info | [55] | |||
8 | Donitriptan | Drug Info | [57] | |||
9 | GR-127935 | Drug Info | [58] | |||
10 | VR-147 | Drug Info | [63], [49] | |||
Antagonist | [+] 12 Antagonist drugs | + | ||||
1 | Metergolin | Drug Info | [38] | |||
2 | BMS-181101 | Drug Info | [52], [49] | |||
3 | Tidembersat | Drug Info | [49] | |||
4 | 9-OH-risperidone | Drug Info | [79] | |||
5 | bufotenine | Drug Info | [76] | |||
6 | L-772,405 | Drug Info | [85] | |||
7 | m-chlorophenylpiperazine | Drug Info | [38] | |||
8 | MPDT | Drug Info | [82] | |||
9 | SB 272183 | Drug Info | [86] | |||
10 | SB 649915 | Drug Info | [87] | |||
11 | SB 714786 | Drug Info | [87] | |||
12 | [3H]GR 125,743 | Drug Info | [90] | |||
Inhibitor | [+] 53 Inhibitor drugs | + | ||||
1 | L-741604 | Drug Info | [60] | |||
2 | L-775606 | Drug Info | [61] | |||
3 | (+/-)-nantenine | Drug Info | [64] | |||
4 | (3-Chloro-phenyl)-piperazin-1-yl-methanone | Drug Info | [65] | |||
5 | 1,2,3,4-Tetrahydro-naphthalen-2-ylamine | Drug Info | [66] | |||
6 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [67] | |||
7 | 1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine | Drug Info | [65] | |||
8 | 1-(2,5-Dimethoxy-phenyl)-piperazine | Drug Info | [65] | |||
9 | 1-(2,5-dimethoxyphenyl)propan-2-amine | Drug Info | [68] | |||
10 | 1-(2-Butoxy-phenyl)-piperazine | Drug Info | [69] | |||
11 | 1-(2-Ethoxy-phenyl)-piperazine | Drug Info | [69] | |||
12 | 1-(2-Fluoro-phenyl)-piperazine | Drug Info | [69] | |||
13 | 1-(2-Isopropoxy-phenyl)-piperazine | Drug Info | [69] | |||
14 | 1-(2-Methoxy-phenyl)-piperazine | Drug Info | [69] | |||
15 | 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [70] | |||
16 | 1-(3-Fluoro-phenyl)-piperazine | Drug Info | [69] | |||
17 | 1-(3-Nitro-phenyl)-piperazine | Drug Info | [69] | |||
18 | 1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine | Drug Info | [65] | |||
19 | 1-(7-Methoxy-naphthalen-2-yl)-piperazine | Drug Info | [71] | |||
20 | 1-Naphthalen-2-yl-piperazine | Drug Info | [66] | |||
21 | 2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole | Drug Info | [73] | |||
22 | 2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol | Drug Info | [68] | |||
23 | 2-(2-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [68] | |||
24 | 2-(3-Methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [68] | |||
25 | 2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine | Drug Info | [68] | |||
26 | 2-(4-Bromo-phenyl)-1-methyl-ethylamine | Drug Info | [68] | |||
27 | 2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole | Drug Info | [73] | |||
28 | 2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine | Drug Info | [74] | |||
29 | 2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine | Drug Info | [75] | |||
30 | 2-Piperazin-1-yl-benzonitrile | Drug Info | [69] | |||
31 | 2-Piperazin-1-yl-phenol | Drug Info | [65] | |||
32 | 3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one | Drug Info | [65] | |||
33 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
34 | 5-amino-3-(N-methylpiperidin-4-yl)-1H-indole | Drug Info | [61] | |||
35 | 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
36 | 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
37 | 5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole | Drug Info | [78] | |||
38 | 5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole | Drug Info | [78] | |||
39 | 8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline | Drug Info | [66] | |||
40 | 8-Methoxy-2-piperazin-1-yl-quinoline | Drug Info | [66] | |||
41 | 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [77] | |||
42 | 8-Methoxy-quinolin-2-ylamine | Drug Info | [66] | |||
43 | AGROCLAVINE | Drug Info | [80] | |||
44 | Brolamfetamine | Drug Info | [68] | |||
45 | CHLOROPHENYLPIPERAZINE | Drug Info | [69] | |||
46 | Etisulergine | Drug Info | [83] | |||
47 | L-747201 | Drug Info | [84] | |||
48 | L-760790 | Drug Info | [60] | |||
49 | PHENYLPIPERAZINE | Drug Info | [66] | |||
50 | QUIPAZINE | Drug Info | [66] | |||
51 | SEROTONIN | Drug Info | [61] | |||
52 | WAY-466 | Drug Info | [88] | |||
53 | [2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine | Drug Info | [78] |
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 | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"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 | Drug information of Almogran, 2008. eduDrugs. | |||||
REF 3 | 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 4 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 5 | 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 6 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 7 | Clinical pipeline report, company report or official report of Intelgenx. | |||||
REF 8 | 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 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 800007062) | |||||
REF 29 | 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 30 | 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 31 | 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 32 | 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 33 | 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 34 | 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 35 | 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 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 | Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8. | |||||
REF 39 | An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. | |||||
REF 40 | 5-Hydroxytryptamine(1F) receptors do not participate in vasoconstriction: lack of vasoconstriction to LY344864, a selective serotonin(1F) receptor agonist in rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):935-9. | |||||
REF 41 | 5-Hydroxytryptamine receptor agonists for the abortive treatment of vascular headaches block mast cell, endothelial and platelet activation within the rat dura mater after trigeminal stimulation. Brain Res. 1992 Jun 26;583(1-2):137-49. | |||||
REF 42 | Novel approaches to the treatment of nausea and vomiting. Dig Dis. 1999;17(3):125-32. | |||||
REF 43 | Serotonin in migraine: theories, animal models and emerging therapies. Prog Drug Res. 1998;51:219-44. | |||||
REF 44 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 45 | Clinical pipeline report, company report or official report of Neurim Pharmaceuticals. | |||||
REF 46 | Company report (NeurAxon) | |||||
REF 47 | Company report (Fabrekramer) | |||||
REF 48 | 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 49 | 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 50 | Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65. | |||||
REF 51 | 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 52 | 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 53 | 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 54 | DOI: 10.1002/9781118541203.xen439 | |||||
REF 55 | 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 56 | 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 57 | 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 58 | GR127935: a potent and selective 5-HT1D receptor antagonist.Behav Brain Res.1996;73(1-2):157-61. | |||||
REF 59 | L-694,247: a potent 5-HT1D receptor agonist. Br J Pharmacol. 1993 Nov;110(3):1196-200. | |||||
REF 60 | 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 61 | 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. | |||||
REF 62 | Role of 5-HT(1) receptor subtypes in the modulation of pain and synaptic transmission in rat spinal superficial dorsal horn. Br J Pharmacol. 2012 Mar;165(6):1956-65. | |||||
REF 63 | US patent application no. 2010,0112,050, Dosage form for insertion into the mouth. | |||||
REF 64 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
REF 65 | Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4. | |||||
REF 66 | 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80. | |||||
REF 67 | 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28. | |||||
REF 68 | 5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. J Med Chem. 1986 Feb;29(2):194-9. | |||||
REF 69 | Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. J Med Chem. 1989 May;32(5):1052-6. | |||||
REF 70 | The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. | |||||
REF 71 | 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem. 1997 Nov 21;40(24):3974-8. | |||||
REF 72 | Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta. Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3630-4. | |||||
REF 73 | 2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4697-9. | |||||
REF 74 | 5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. J Med Chem. 1994 Sep 2;37(18):2828-30. | |||||
REF 75 | 5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine. Bioorg Med Chem Lett. 2000 May 1;10(9):903-5. | |||||
REF 76 | Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Mol Pharmacol. 1996 Dec;50(6):1567-80. | |||||
REF 77 | Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. | |||||
REF 78 | 5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists. Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9. | |||||
REF 79 | 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 80 | Ergolines as selective 5-HT1 agonists. J Med Chem. 1988 Aug;31(8):1512-9. | |||||
REF 81 | SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20. | |||||
REF 82 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8. | |||||
REF 83 | Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-... J Med Chem. 1985 Oct;28(10):1540-2. | |||||
REF 84 | Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1997 Oct 24;40(22):3501-3. | |||||
REF 85 | 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem. 1999 Dec 2;42(24):4981-5001. | |||||
REF 86 | SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue. Br J Pharmacol. 2001 Jul;133(6):797-806. | |||||
REF 87 | Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem. 2005 May 19;48(10):3478-80. | |||||
REF 88 | Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6. | |||||
REF 89 | Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain. Naunyn Schmiedebergs Arch Pharmacol. 1993 Jun;347(6):569-82. | |||||
REF 90 | Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett. 1999 Jul 30;456(1):63-7. | |||||
REF 91 | Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1999 Jun;359(6):447-53. | |||||
REF 92 | Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.