Target Information

Target General Infomation
Target ID
T78656
Former ID
TTDR01194
Target Name
5-hydroxytryptamine 1F receptor
Gene Name
HTR1F
Synonyms
5-HT-1F; 5-HT1F receptor; Serotonin receptor; Serotonin receptor 1F; HTR1F
Target Type
Clinical Trial
Disease Migraine [ICD9: 346; ICD10: G43]
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and 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.
BioChemical Class
GPCR rhodopsin
Target Validation
T78656
UniProt ID
P30939
Sequence
MDFLNSSDQNLTSEELLNRMPSKILVSLTLSGLALMTTTINSLVIAAIIVTRKLHHPANY
LICSLAVTDFLVAVLVMPFSIVYIVRESWIMGQVVCDIWLSVDITCCTCSILHLSAIALD
RYRAITDAVEYARKRTPKHAGIMITIVWIISVFISMPPLFWRHQGTSRDDECIIKHDHIV
STIYSTFGAFYIPLALILILYYKIYRAAKTLYHKRQASRIAKEEVNGQVLLESGEKSTKS
VSTSYVLEKSLSDPSTDFDKIHSTVRSLRSEFKHEKSWRRQKISGTRERKAATTLGLILG
AFVICWLPFFVKELVVNVCDKCKISEEMSNFLAWLGYLNSLINPLIYTIFNEDFKKAFQK
LVRCRC
Drugs and Mode of Action
Drug(s) Lasmiditan Drug Info Phase 3 Migraine [532737], [540550]
LY-334370 Drug Info Phase 2 Migraine [534655], [539288]
Antagonist 1-naphthylpiperazine Drug Info [534427]
metergoline Drug Info [534427]
Agonist 2-methyl-5-HT Drug Info [534001]
5-BODMT Drug Info [531404]
5-CT Drug Info [534427]
alpha-methyl-5-HT Drug Info [534001]
BRL-15572 Drug Info [534475]
dipropyl-5-CT Drug Info [534001]
Lasmiditan Drug Info [532737]
LY344864 Drug Info [534894]
TFMPP Drug Info [534001]
[125I]LSD Drug Info [526750]
Modulator LY-334370 Drug Info
Inhibitor WAY-466 Drug Info [527381]
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
GPCRs, Other
References
Ref 532737Emerging therapeutic options for acute migraine: focus on the potential of lasmiditan. Neuropsychiatr Dis Treat. 2014 Mar 31;10:547-52.
Ref 534655G-protein activation at 5-HT1A receptors by the 5-ht1F ligand LY334370 in guinea-pig brain sections and recombinant cell lines. Br J Pharmacol. 1998 May;124(2):283-90.
Ref 539288(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: 20).
Ref 540550(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: 3928).
Ref 526750Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. J Biol Chem. 1992 Oct 5;267(28):19761-4.
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 531404Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-7.
Ref 532737Emerging therapeutic options for acute migraine: focus on the potential of lasmiditan. Neuropsychiatr Dis Treat. 2014 Mar 31;10:547-52.
Ref 534001Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci U S A. 1993 Jan 15;90(2):408-12.
Ref 534427Cloning and characterization of the guinea pig 5-HT1F receptor subtype: a comparison of the pharmacological profile to the human species homolog. Neuropharmacology. 1997 Apr-May;36(4-5):569-76.
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 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.

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