Target Information

Target General Infomation
Target ID
T11072
Former ID
TTDS00100
Target Name
5-hydroxytryptamine 1D receptor
Gene Name
HTR1D
Synonyms
5-HT-1D; 5-HT-1D-alpha; 5-HT1D receptor; 5-hydroxytryptamine receptor 1D; 5HT1D; Serotonin receptor; Serotonin receptor 1D; HTR1D
Target Type
Successful
Disease Acute migraine [ICD9: 346; ICD10: G43]
Epilepsy [ICD10: G40]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Migraine headaches [ICD9: 346; ICD10: G43]
Migraine [ICD9: 346; ICD10: G43]
Mood disorder [ICD10: F30-F39]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Severe mood disorders [ICD9: 296; ICD10: F30-F39]
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also 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.
BioChemical Class
GPCR rhodopsin
Target Validation
T11072
UniProt ID
P28221
Sequence
MSPLNQSAEGLPQEASNRSLNATETSEAWDPRTLQALKISLAVVLSVITLATVLSNAFVL
TTILLTRKLHTPANYLIGSLATTDLLVSILVMPISIAYTITHTWNFGQILCDIWLSSDIT
CCTASILHLCVIALDRYWAITDALEYSKRRTAGHAATMIAIVWAISICISIPPLFWRQAK
AQEEMSDCLVNTSQISYTIYSTCGAFYIPSVLLIILYGRIYRAARNRILNPPSLYGKRFT
TAHLITGSAGSSLCSLNSSLHEGHSHSAGSPLFFNHVKIKLADSALERKRISAARERKAT
KILGIILGAFIICWLPFFVVSLVLPICRDSCWIHPALFDFFTWLGYLNSLINPIIYTVFN
EEFRQAFQKIVPFRKAS
Drugs and Mode of Action
Drug(s) Almogran Drug Info Approved Migraine [1]
Dihydroergotamine nasal Drug Info Approved Migraine [2]
Eletriptan Drug Info Approved Migraine [3], [4]
Frovatriptan Drug Info Approved Migraine headaches [3], [5]
Rizatriptan Drug Info Approved Acute migraine [6], [7]
Sumatriptan Drug Info Approved Migraine headaches [3], [8]
Zolmitriptan Drug Info Approved Migraine [9], [10]
Neu-P11 Drug Info Phase 2 Insomnia [11]
NXN-188 Drug Info Phase 2 Migraine [12]
TGBA01AD Drug Info Phase 2 Severe mood disorders [13]
Tonabersat Drug Info Phase 2 Epilepsy [14]
Donitriptan Drug Info Preclinical Migraine [15], [16]
Alniditan Drug Info Discontinued in Phase 3 Migraine [17], [18]
Avitriptan Drug Info Discontinued in Phase 3 Migraine [19]
BMS-181101 Drug Info Discontinued in Phase 2 Mood disorder [20], [21]
CP-122288 Drug Info Discontinued in Phase 2 Migraine [22], [23]
Elzasonan hydrochloride Drug Info Discontinued in Phase 2 Severe mood disorders [13]
IS-159 Drug Info Discontinued in Phase 2 Migraine [24]
PNU-142633 Drug Info Discontinued in Phase 2 Migraine [25]
ALX-0646 Drug Info Discontinued in Phase 1 Migraine [26]
Tidembersat Drug Info Discontinued in Phase 1 Migraine [27]
BMS-181885 Drug Info Terminated Migraine [28]
GR-127935 Drug Info Terminated Major depressive disorder [29], [30]
L-694247 Drug Info Terminated Migraine [31], [32]
L-741604 Drug Info Terminated Discovery agent [33]
L-775606 Drug Info Terminated Discovery agent [34], [35]
PNU-109291 Drug Info Terminated Migraine [36], [37]
VR-147 Drug Info Terminated Migraine [38]
Inhibitor (+/-)-nantenine Drug Info [39]
(3-Chloro-phenyl)-piperazin-1-yl-methanone Drug Info [40]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info [41]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [42]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info [40]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info [40]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info [43]
1-(2-Butoxy-phenyl)-piperazine Drug Info [44]
1-(2-Ethoxy-phenyl)-piperazine Drug Info [44]
1-(2-Fluoro-phenyl)-piperazine Drug Info [44]
1-(2-Isopropoxy-phenyl)-piperazine Drug Info [44]
1-(2-Methoxy-phenyl)-piperazine Drug Info [44]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [45]
1-(3-Fluoro-phenyl)-piperazine Drug Info [44]
1-(3-Nitro-phenyl)-piperazine Drug Info [44]
1-(3-Trifluoromethyl-phenyl)-piperazine Drug Info [40]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info [40]
1-(7-Methoxy-naphthalen-2-yl)-piperazine Drug Info [46]
1-Naphthalen-1-yl-piperazine Drug Info [41]
1-Naphthalen-2-yl-piperazine Drug Info [41]
2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole Drug Info [47]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info [43]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [43]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [43]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info [43]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info [43]
2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole Drug Info [47]
2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine Drug Info [48]
2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine Drug Info [49]
2-Piperazin-1-yl-benzonitrile Drug Info [44]
2-Piperazin-1-yl-phenol Drug Info [40]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info [40]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [50]
5-amino-3-(N-methylpiperidin-4-yl)-1H-indole Drug Info [51]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [50]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [50]
5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole Drug Info [52]
5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole Drug Info [52]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info [41]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info [41]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [50]
8-Methoxy-quinolin-2-ylamine Drug Info [41]
AGROCLAVINE Drug Info [53]
Brolamfetamine Drug Info [43]
CHLOROPHENYLPIPERAZINE Drug Info [44]
Etisulergine Drug Info [54]
L-741604 Drug Info [55]
L-747201 Drug Info [56]
L-760790 Drug Info [55]
L-775606 Drug Info [51]
PHENYLPIPERAZINE Drug Info [41]
QUIPAZINE Drug Info [41]
SEROTONIN Drug Info [51]
WAY-466 Drug Info [57]
[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info [52]
Agonist 1-naphthylpiperazine Drug Info [58]
2-methyl-5-HT Drug Info [59]
5-CT Drug Info [60]
7-methoxy-1-naphthylpiperazine Drug Info [46]
Almogran Drug Info [61]
Alniditan Drug Info [62], [2]
alpha-methyl-5-HT Drug Info [59]
ALX-0646 Drug Info [2]
Avitriptan Drug Info [63], [2]
BMS-181885 Drug Info [64], [2]
BRL-15572 Drug Info [65]
CP-122288 Drug Info [66], [2]
dipropyl-5-CT Drug Info [58]
EMDT Drug Info [67]
L-694247 Drug Info [68], [2]
lysergic acid Drug Info [59]
lysergol Drug Info [58]
Neu-P11 Drug Info [69]
PNU-109291 Drug Info [70], [2]
PNU-142633 Drug Info [71], [2]
Rizatriptan Drug Info [72]
SB 216641 Drug Info [65]
Sumatriptan Drug Info [73], [74], [75], [76], [77]
TFMPP Drug Info [60]
Tonabersat Drug Info [78], [2]
[125I]GTI Drug Info [79]
[3H]5-CT Drug Info [80]
[3H]5-HT Drug Info [62]
[3H]8-OH-DPAT Drug Info [81]
[3H]alniditan Drug Info [62]
[3H]eletriptan Drug Info [82]
[3H]sumatriptan Drug Info [82]
Antagonist 9-OH-risperidone Drug Info [83]
BMS-181101 Drug Info [64], [2]
bufotenine Drug Info [59]
L-772,405 Drug Info [84]
m-chlorophenylpiperazine Drug Info [60]
metergoline Drug Info [60]
MPDT Drug Info [67]
SB 272183 Drug Info [85]
SB 649915 Drug Info [86]
SB 714786 Drug Info [86]
Tidembersat Drug Info [2]
[3H]GR 125,743 Drug Info [80]
Modulator Dihydroergotamine nasal Drug Info [62]
Donitriptan Drug Info
Eletriptan Drug Info [87]
Elzasonan hydrochloride Drug Info
Frovatriptan Drug Info [87]
GR-127935 Drug Info
IS-159 Drug Info
NXN-188 Drug Info
TGBA01AD Drug Info
VR-147 Drug Info [88], [2]
Zolmitriptan Drug Info [87]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
Serotonergic synapse
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
5HT1 type receptor mediated signaling pathway
Reactome Serotonin receptors
G alpha (i) signalling events
WikiPathways Serotonin HTR1 Group and FOS Pathway
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
REF 1Drug information of Almogran, 2008. eduDrugs.
REF 2Sustained 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 3Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
REF 4(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 5(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(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: 51).
REF 7FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077263.
REF 8(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 9FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020768.
REF 10(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 11ClinicalTrials.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 12ClinicalTrials.gov (NCT00920686) Study of NXN 188 for the Treatment of Migraine With Aura. U.S. National Institutes of Health.
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REF 14ClinicalTrials.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(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 16Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012002)
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REF 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006286)
REF 19Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002927)
REF 20(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 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005177)
REF 22(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 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005787)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005786)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013927)
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008400)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010348)
REF 28Trusted, 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(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 30Trusted, 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(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 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003457)
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REF 35Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009132)
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REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010481)
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