Target Information
| Target General Information | Top | |||||
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| Target ID |
T07806
(Former ID: TTDS00099)
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| Target Name |
5-HT 1B receptor (HTR1B)
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| Synonyms |
Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
Click to Show/Hide
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| Gene Name |
HTR1B
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Migraine [ICD-11: 8A80] | |||||
| 2 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
| 3 | Psychotic disorder [ICD-11: 6A20-6A25] | |||||
| 4 | Schizophrenia [ICD-11: 6A20] | |||||
| Function |
Functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). 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. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries. 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 |
MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALIT
LATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQV VCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISI SLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRIL KQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLE KKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYL NSLINPIIYTMSNEDFKQAFHKLIRFKCTS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T97ZTQ | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 7 Approved Drugs | + | ||||
| 1 | Eletriptan | Drug Info | Approved | Migraine | [2], [3] | |
| 2 | Fluphenazine | Drug Info | Approved | Psychotic disorder | [4], [5] | |
| 3 | Frovatriptan | Drug Info | Approved | Migraine | [3], [6] | |
| 4 | Metergolin | Drug Info | Approved | Hyperprolactinaemia | [7] | |
| 5 | Naratriptan | Drug Info | Approved | Migraine | [3], [8] | |
| 6 | Prolixin decanoate | Drug Info | Approved | Schizophrenia | [9] | |
| 7 | Zolmitriptan | Drug Info | Approved | Migraine | [10], [11] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | Eltoprazine | Drug Info | Phase 3 | Attention deficit hyperactivity disorder | [12] | |
| 2 | NXN-188 | Drug Info | Phase 2 | Migraine | [13] | |
| 3 | [N-methyl-3H(3)]AZ-10419369 | Drug Info | Phase 1 | Mood disorder | [14], [15] | |
| Discontinued Drug(s) | [+] 9 Discontinued Drugs | + | ||||
| 1 | Alniditan | Drug Info | Discontinued in Phase 3 | Migraine | [16], [17] | |
| 2 | Elzasonan hydrochloride | Drug Info | Discontinued in Phase 2 | Mood disorder | [18] | |
| 3 | IS-159 | Drug Info | Discontinued in Phase 2 | Migraine | [19] | |
| 4 | Anpirtoline | Drug Info | Terminated | Pain | [22] | |
| 5 | AZD-1134 | Drug Info | Terminated | Anxiety disorder | [23] | |
| 6 | CGS-12066B | Drug Info | Terminated | Anxiety disorder | [24], [25] | |
| 7 | F-12682 | Drug Info | Terminated | Major depressive disorder | [26] | |
| 8 | GR-127935 | Drug Info | Terminated | Major depressive disorder | [27], [28] | |
| 9 | VR-147 | Drug Info | Terminated | Migraine | [29] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | Donitriptan | Drug Info | Preclinical | Migraine | [20], [21] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Modulator | [+] 13 Modulator drugs | + | ||||
| 1 | Eletriptan | Drug Info | [30] | |||
| 2 | Fluphenazine | Drug Info | [30] | |||
| 3 | Frovatriptan | Drug Info | [30] | |||
| 4 | Prolixin decanoate | Drug Info | [30] | |||
| 5 | Zolmitriptan | Drug Info | [30] | |||
| 6 | NXN-188 | Drug Info | [34] | |||
| 7 | Elzasonan hydrochloride | Drug Info | [37] | |||
| 8 | IS-159 | Drug Info | [38] | |||
| 9 | Donitriptan | Drug Info | [39] | |||
| 10 | Anpirtoline | Drug Info | [22] | |||
| 11 | CGS-12066B | Drug Info | [41] | |||
| 12 | GR-127935 | Drug Info | [43] | |||
| 13 | VR-147 | Drug Info | [33], [45] | |||
| Antagonist | [+] 15 Antagonist drugs | + | ||||
| 1 | Metergolin | Drug Info | [31] | |||
| 2 | [N-methyl-3H(3)]AZ-10419369 | Drug Info | [33], [35] | |||
| 3 | AZD-1134 | Drug Info | [33], [40] | |||
| 4 | F-12682 | Drug Info | [33], [42] | |||
| 5 | (R)-flurocarazolol | Drug Info | [47] | |||
| 6 | (S)-flurocarazolol | Drug Info | [47] | |||
| 7 | 5-OH-DPAT | Drug Info | [54] | |||
| 8 | 9-OH-risperidone | Drug Info | [56] | |||
| 9 | GR55562 | Drug Info | [60] | |||
| 10 | SB 224289 | Drug Info | [60] | |||
| 11 | SB 272183 | Drug Info | [62] | |||
| 12 | SB 649915 | Drug Info | [63] | |||
| 13 | SB 714786 | Drug Info | [63] | |||
| 14 | SB236057 | Drug Info | [64], [65] | |||
| 15 | [3H]GR 125,743 | Drug Info | [71] | |||
| Agonist | [+] 20 Agonist drugs | + | ||||
| 1 | Naratriptan | Drug Info | [1] | |||
| 2 | Eltoprazine | Drug Info | [32], [33] | |||
| 3 | Alniditan | Drug Info | [36] | |||
| 4 | 1-naphthylpiperazine | Drug Info | [31] | |||
| 5 | 2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine | Drug Info | [50] | |||
| 6 | 2-methyl-5-HT | Drug Info | [52] | |||
| 7 | 5-CT | Drug Info | [54] | |||
| 8 | 7-methoxy-1-naphthylpiperazine | Drug Info | [49] | |||
| 9 | BRL-15572 | Drug Info | [58] | |||
| 10 | CP-94,253 | Drug Info | [59] | |||
| 11 | dipropyl-5-CT | Drug Info | [52] | |||
| 12 | L-772,405 | Drug Info | [61] | |||
| 13 | lysergol | Drug Info | [31] | |||
| 14 | SB 216641 | Drug Info | [58] | |||
| 15 | TFMPP | Drug Info | [31] | |||
| 16 | [11C]AZ10419369 | Drug Info | [67] | |||
| 17 | [125I]GTI | Drug Info | [68] | |||
| 18 | [3H]8-OH-DPAT | Drug Info | [69] | |||
| 19 | [3H]eletriptan | Drug Info | [70] | |||
| 20 | [3H]sumatriptan | Drug Info | [70] | |||
| Inhibitor | [+] 14 Inhibitor drugs | + | ||||
| 1 | L-775606 | Drug Info | [44] | |||
| 2 | (+/-)-nantenine | Drug Info | [46] | |||
| 3 | 1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine | Drug Info | [48] | |||
| 4 | 1-(7-Methoxy-naphthalen-2-yl)-piperazine | Drug Info | [49] | |||
| 5 | 1-Naphthalen-2-yl-piperazine | Drug Info | [49] | |||
| 6 | 2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine | Drug Info | [51] | |||
| 7 | 5-amino-3-(N-methylpiperidin-4-yl)-1H-indole | Drug Info | [53] | |||
| 8 | 5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole | Drug Info | [55] | |||
| 9 | 5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole | Drug Info | [55] | |||
| 10 | A-987306 | Drug Info | [57] | |||
| 11 | L-747201 | Drug Info | [44] | |||
| 12 | SEROTONIN | Drug Info | [57] | |||
| 13 | WAY-466 | Drug Info | [66] | |||
| 14 | [2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine | Drug Info | [55] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Ergotamine | Ligand Info | |||||
| Structure Description | Crystal structure of the chimeric protein of 5-HT1B-BRIL in complex with ergotamine (PSI Community Target) | PDB:4IAR | ||||
| Method | X-ray diffraction | Resolution | 2.70 Å | Mutation | Yes | [72] |
| PDB Sequence |
YIYQDSISLP
47 WKVLLVMLLA57 LITLATTLSN67 AFVIATVYRT77 RKLHTPANYL87 IASLAVTDLL 97 VSILVMPIST107 MYTVTGRWTL117 GQVVCDFWLS127 SDITCCTASI137 WHLCVIALDR 147 YWAITDAVEY157 SAKRTPKRAA167 VMIALVWVFS177 ISISLPPFFW187 RQASECVVNT 203 DHILYTVYST213 VGAFYFPTLL223 LIALYGRIYV233 EARSRIADLE1004 DNWETLNDNL 1014 KVIEKADNAA1024 QVKDALTKMR1034 AAALDAQKAT1044 PPKLEDKSPD1054 SPEMKDFRHG 1064 FDILVGQIDD1074 ALKLANEGKV1084 KEAQAAAEQL1094 KTTRNAYIQK1104 YLAARERKAT 313 KTLGIILGAF323 IVCWLPFFII333 SLVMPIWFHL348 AIFDFFTWLG358 YLNSLINPII 368 YTMSNEDFKQ378 AFHKLIRFK
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TYR109
4.445
TRP125
3.919
LEU126
3.717
ASP129
2.722
ILE130
3.477
CYS133
3.354
THR134
2.945
ILE137
4.533
ILE180
4.755
CYS199
3.334
VAL200
3.450
VAL201
3.208
THR203
4.973
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Dihydroergotamine | Ligand Info | |||||
| Structure Description | Crystal structure of the chimeric protein of 5-HT1B-BRIL in complex with dihydroergotamine (PSI Community Target) | PDB:4IAQ | ||||
| Method | X-ray diffraction | Resolution | 2.80 Å | Mutation | Yes | [72] |
| PDB Sequence |
YIYQDSISLP
47 WKVLLVMLLA57 LITLATTLSN67 AFVIATVYRT77 RKLHTPANYL87 IASLAVTDLL 97 VSILVMPIST107 MYTVTGRWTL117 GQVVCDFWLS127 SDITCCTASI137 WHLCVIALDR 147 YWAITDAVEY157 SAKRTPKRAA167 VMIALVWVFS177 ISISLPPFFW187 RQASECVVNT 203 DHILYTVYST213 VGAFYFPTLL223 LIALYGRIYV233 EARSRIADLE1004 DNWETLNDNL 1014 KVINAAQVKD1028 ALTKMRAAAL1038 DAQKATPDSP1056 EMKDFRHGFD1066 ILVGQIDDAL 1076 KLANEGKVKE1086 AQAAAEQLKT1096 TRNAYIQKYL1106 LMAARERKAT313 KTLGIILGAF 323 IVCWLPFFII333 SLVMPIHLAI350 FDFFTWLGYL360 NSLINPIIYT370 MSNEDFKQAF 380 HKLIRFK
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TYR109
4.276
TRP125
3.993
LEU126
3.844
ASP129
3.004
ILE130
3.484
CYS133
3.414
THR134
2.778
ILE137
4.908
ILE180
4.528
CYS199
3.078
VAL200
3.393
VAL201
3.011
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| 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).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| 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 | ||
| Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 0.00E+00 |
|---|---|---|---|---|---|
| Closeness centrality | 1.91E-01 | Radiality | 1.33E+01 | Clustering coefficient | 1.00E+00 |
| Neighborhood connectivity | 3.20E+01 | Topological coefficient | 6.81E-01 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (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 | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| 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 | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9. | |||||
| 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: 40). | |||||
| 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 | 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: 204). | |||||
| REF 5 | The antipsychotic drug, fluphenazine, effectively reverses mechanical allodynia in rat models of neuropathic pain. Psychopharmacology (Berl). 2008 Jan;195(4):559-68. | |||||
| 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: 7191). | |||||
| REF 7 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| 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: 45). | |||||
| REF 9 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 016727. | |||||
| REF 10 | 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 11 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020768. | |||||
| REF 12 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 13 | ClinicalTrials.gov (NCT00920686) Study of NXN 188 for the Treatment of Migraine With Aura. U.S. National Institutes of Health. | |||||
| REF 14 | 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: 3219). | |||||
| REF 15 | ClinicalTrials.gov (NCT01085123) Determine Central 5-HT1B Receptor Occupancy of ZOMIG Rapimelt (Zolmitriptan) in Healthy Male Volunteers. U.S. National Institutes of Health. | |||||
| REF 16 | 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 17 | 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 18 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
| 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 800005786) | |||||
| 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: 39). | |||||
| 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 800012002) | |||||
| REF 22 | Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study. Nucl Med Biol. 2006 Apr;33(3):325-32. | |||||
| 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 800017898) | |||||
| REF 24 | 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: 109). | |||||
| 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 800006033) | |||||
| REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010898) | |||||
| REF 27 | 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 28 | 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 29 | 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 30 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 31 | Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem. 1996 Nov;67(5):2096-103. | |||||
| REF 32 | Clinical pipeline report, company report or official report of Jazz Pharmaceuticals. | |||||
| REF 33 | 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 34 | Company report (NeurAxon) | |||||
| REF 35 | 5-HT1B and other related serotonergic proteins are altered in APPswe mutation. Neurosci Lett. 2015 May 6;594:137-43. | |||||
| REF 36 | 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 37 | DOI: 10.1002/9781118541203.xen439 | |||||
| REF 38 | 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 39 | 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 40 | N-methyl-3H3AZ10419369 binding to the 5-HT1B receptor: in vitro characterization and in vivo receptor occupancy. J Pharmacol Exp Ther. 2009 Jul;330(1):342-51. | |||||
| REF 41 | Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist. Eur J Pharmacol. 1987 Apr 7;136(1):1-9. | |||||
| REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010898) | |||||
| REF 43 | GR127935: a potent and selective 5-HT1D receptor antagonist.Behav Brain Res.1996;73(1-2):157-61. | |||||
| REF 44 | Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1997 Oct 24;40(22):3501-3. | |||||
| REF 45 | US patent application no. 2010,0112,050, Dosage form for insertion into the mouth. | |||||
| REF 46 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
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