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 [550661]
Dihydroergotamine nasal Drug Info Approved Migraine [551730]
Eletriptan Drug Info Approved Migraine [536361], [540615]
Frovatriptan Drug Info Approved Migraine headaches [536361], [542203]
Rizatriptan Drug Info Approved Acute migraine [468161], [538326]
Sumatriptan Drug Info Approved Migraine headaches [536361], [540805]
Zolmitriptan Drug Info Approved Migraine [538555], [541265]
Neu-P11 Drug Info Phase 2 Insomnia [523722]
NXN-188 Drug Info Phase 2 Migraine [522692]
TGBA01AD Drug Info Phase 2 Severe mood disorders [536580]
Tonabersat Drug Info Phase 2 Epilepsy [522123]
Donitriptan Drug Info Preclinical Migraine [540538], [547009]
Alniditan Drug Info Discontinued in Phase 3 Migraine [538712], [546088]
Avitriptan Drug Info Discontinued in Phase 3 Migraine [545344]
BMS-181101 Drug Info Discontinued in Phase 2 Mood disorder [538662], [545877]
CP-122288 Drug Info Discontinued in Phase 2 Migraine [538675], [545996]
Elzasonan hydrochloride Drug Info Discontinued in Phase 2 Severe mood disorders [536580]
IS-159 Drug Info Discontinued in Phase 2 Migraine [545995]
PNU-142633 Drug Info Discontinued in Phase 2 Migraine [547202]
ALX-0646 Drug Info Discontinued in Phase 1 Migraine [546474]
Tidembersat Drug Info Discontinued in Phase 1 Migraine [546798]
BMS-181885 Drug Info Terminated Migraine [546243]
GR-127935 Drug Info Terminated Major depressive disorder [538876], [545301]
L-694247 Drug Info Terminated Migraine [538938], [545490]
L-741604 Drug Info Terminated Discovery agent [546098]
L-775606 Drug Info Terminated Discovery agent [538680], [546600]
PNU-109291 Drug Info Terminated Migraine [540203], [546823]
VR-147 Drug Info Terminated Migraine [548264]
Inhibitor (+/-)-nantenine Drug Info [530558]
(3-Chloro-phenyl)-piperazin-1-yl-methanone Drug Info [533476]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info [533482]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [527952]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info [533476]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info [533476]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info [533498]
1-(2-Butoxy-phenyl)-piperazine Drug Info [533134]
1-(2-Ethoxy-phenyl)-piperazine Drug Info [533134]
1-(2-Fluoro-phenyl)-piperazine Drug Info [533134]
1-(2-Isopropoxy-phenyl)-piperazine Drug Info [533134]
1-(2-Methoxy-phenyl)-piperazine Drug Info [533134]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [529013]
1-(3-Fluoro-phenyl)-piperazine Drug Info [533134]
1-(3-Nitro-phenyl)-piperazine Drug Info [533134]
1-(3-Trifluoromethyl-phenyl)-piperazine Drug Info [533476]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info [533476]
1-(7-Methoxy-naphthalen-2-yl)-piperazine Drug Info [534528]
1-Naphthalen-1-yl-piperazine Drug Info [533482]
1-Naphthalen-2-yl-piperazine Drug Info [533482]
2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazole Drug Info [527180]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info [533498]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole Drug Info [527180]
2-(5-Nonyloxy-1H-indol-3-yl)-ethylamine Drug Info [533876]
2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine Drug Info [525792]
2-Piperazin-1-yl-benzonitrile Drug Info [533134]
2-Piperazin-1-yl-phenol Drug Info [533476]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info [533476]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-amino-3-(N-methylpiperidin-4-yl)-1H-indole Drug Info [529496]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole Drug Info [525845]
5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole Drug Info [525845]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info [533482]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info [533482]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [529148]
8-Methoxy-quinolin-2-ylamine Drug Info [533482]
AGROCLAVINE Drug Info [532683]
Brolamfetamine Drug Info [533498]
CHLOROPHENYLPIPERAZINE Drug Info [533134]
Etisulergine Drug Info [533501]
L-741604 Drug Info [525431]
L-747201 Drug Info [534500]
L-760790 Drug Info [525431]
L-775606 Drug Info [529496]
PHENYLPIPERAZINE Drug Info [533482]
QUIPAZINE Drug Info [533482]
SEROTONIN Drug Info [529496]
WAY-466 Drug Info [527381]
[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info [525845]
Agonist 1-naphthylpiperazine Drug Info [527380]
2-methyl-5-HT Drug Info [534292]
5-CT Drug Info [528072]
7-methoxy-1-naphthylpiperazine Drug Info [534528]
Almogran Drug Info [535330]
Alniditan Drug Info [534635], [551730]
alpha-methyl-5-HT Drug Info [534292]
ALX-0646 Drug Info [551730]
Avitriptan Drug Info [534756], [551730]
BMS-181885 Drug Info [525577], [551730]
BRL-15572 Drug Info [534475]
CP-122288 Drug Info [534381], [551730]
dipropyl-5-CT Drug Info [527380]
EMDT Drug Info [525722]
L-694247 Drug Info [533978], [551730]
lysergic acid Drug Info [534292]
lysergol Drug Info [527380]
Neu-P11 Drug Info [551415]
PNU-109291 Drug Info [531636], [551730]
PNU-142633 Drug Info [526906], [551730]
Rizatriptan Drug Info [535607]
SB 216641 Drug Info [534475]
Sumatriptan Drug Info [534894], [534966], [535146], [535803], [538154]
TFMPP Drug Info [528072]
Tonabersat Drug Info [525903], [551730]
[125I]GTI Drug Info [533994]
[3H]5-CT Drug Info [525563]
[3H]5-HT Drug Info [534635]
[3H]8-OH-DPAT Drug Info [525553]
[3H]alniditan Drug Info [534635]
[3H]eletriptan Drug Info [525461]
[3H]sumatriptan Drug Info [525461]
Antagonist 9-OH-risperidone Drug Info [534281]
BMS-181101 Drug Info [525577], [551730]
bufotenine Drug Info [534292]
L-772,405 Drug Info [525646]
m-chlorophenylpiperazine Drug Info [528072]
metergoline Drug Info [528072]
MPDT Drug Info [525722]
SB 272183 Drug Info [526100]
SB 649915 Drug Info [527551]
SB 714786 Drug Info [527551]
Tidembersat Drug Info [551730]
[3H]GR 125,743 Drug Info [525563]
Modulator Dihydroergotamine nasal Drug Info [534635]
Donitriptan Drug Info
Eletriptan Drug Info [556264]
Elzasonan hydrochloride Drug Info
Frovatriptan Drug Info [556264]
GR-127935 Drug Info
IS-159 Drug Info
NXN-188 Drug Info
TGBA01AD Drug Info
VR-147 Drug Info [550903], [551730]
Zolmitriptan Drug Info [556264]
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
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Ref 522123ClinicalTrials.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 522692ClinicalTrials.gov (NCT00920686) Study of NXN 188 for the Treatment of Migraine With Aura. U.S. National Institutes of Health.
Ref 523722ClinicalTrials.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 536361Natural 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 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 538326FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 077263.
Ref 538555FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020768.
Ref 538662(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 538675(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 538680(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: 114).
Ref 538712(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 538876(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 538938(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 540203(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 540538(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 540615(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 540805(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 541265(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 542203(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).
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Ref 525563Serotonin 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 525577Sensitive 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 5256463-[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 5257222-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
Ref 525792Bioorg Med Chem Lett. 2000 May 1;10(9):903-5.5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.
Ref 525845Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
Ref 525903The 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 526100SB-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 526906Further characterization of the 5-HT1 receptors mediating cardiac sympatho-inhibition in pithed rats: pharmacological correlation with the 5-HT1B and 5-HT1D subtypes. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):220-7. Epub 2003 Dec 12.
Ref 527180Bioorg Med Chem Lett. 2004 Sep 20;14(18):4697-9.2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.
Ref 527380Human 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 527381J Med Chem. 2005 Jan 27;48(2):353-6.Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Ref 527551Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem. 2005 May 19;48(10):3478-80.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 528072Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8.
Ref 529013Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. Epub 2007 Aug 15.The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine.
Ref 529148Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.
Ref 529496J Med Chem. 2008 Jun 26;51(12):3609-16. Epub 2008 May 29.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-piperidinyl)-1H-indol-5-yl]benzamide.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 531636Role 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 532683J Med Chem. 1988 Aug;31(8):1512-9.Ergolines as selective 5-HT1 agonists.
Ref 533134J Med Chem. 1989 May;32(5):1052-6.Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.
Ref 533476J Med Chem. 1986 May;29(5):630-4.Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents.
Ref 533482J Med Chem. 1986 Nov;29(11):2375-80.5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
Ref 533498J Med Chem. 1986 Feb;29(2):194-9.5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues.
Ref 533501J Med Chem. 1985 Oct;28(10):1540-2.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-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
Ref 533876J Med Chem. 1994 Sep 2;37(18):2828-30.5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
Ref 533978L-694,247: a potent 5-HT1D receptor agonist. Br J Pharmacol. 1993 Nov;110(3):1196-200.
Ref 533994Autoradiographic 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 534281Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
Ref 534292Alniditan, 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 534381The 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 534475SB-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 534500J Med Chem. 1997 Oct 24;40(22):3501-3.Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
Ref 534528J Med Chem. 1997 Nov 21;40(24):3974-8.5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
Ref 534635Br J Pharmacol. 1998 Apr;123(8):1655-65.Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines.
Ref 534756Safety 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 5348945-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 534966Novel approaches to the treatment of nausea and vomiting. Dig Dis. 1999;17(3):125-32.
Ref 535146Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
Ref 535330Efficacy 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 535607An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.
Ref 5358035-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 538154Serotonin in migraine: theories, animal models and emerging therapies. Prog Drug Res. 1998;51:219-44.
Ref 550903US patent application no. 2010,0112,050, Dosage form for insertion into the mouth.
Ref 551415Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
Ref 551730Sustained 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 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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