Target Information

Target General Infomation
Target ID
T78656 (Former ID: TTDR01194)
Target Name
5-HT 1F receptor (HTR1F)
Synonyms
Serotonin receptor 1F; HTR1EL; 5-hydroxytryptamine receptor 1F; 5-HT1F receptor; 5-HT1F; 5-HT-1F
Gene Name
HTR1F
Target Type
Successful target
 [1]
Disease [+] 1 Target-related Diseases +
1 Pituitary gland disorder [ICD-11: 5A60-5A61]
Function
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. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
BioChemical Class
GPCR rhodopsin
UniProt ID
5HT1F_HUMAN
Sequence
MDFLNSSDQNLTSEELLNRMPSKILVSLTLSGLALMTTTINSLVIAAIIVTRKLHHPANY
LICSLAVTDFLVAVLVMPFSIVYIVRESWIMGQVVCDIWLSVDITCCTCSILHLSAIALD
RYRAITDAVEYARKRTPKHAGIMITIVWIISVFISMPPLFWRHQGTSRDDECIIKHDHIV
STIYSTFGAFYIPLALILILYYKIYRAAKTLYHKRQASRIAKEEVNGQVLLESGEKSTKS
VSTSYVLEKSLSDPSTDFDKIHSTVRSLRSEFKHEKSWRRQKISGTRERKAATTLGLILG
AFVICWLPFFVKELVVNVCDKCKISEEMSNFLAWLGYLNSLINPLIYTIFNEDFKKAFQK
LVRCRC
Drugs and Modes of Action
Approved Drug(s) [+] 1 Approved Drugs +
1 Metergolin Drug Info Approved Hyperprolactinaemia [2]
Clinical Trial Drug(s) [+] 2 Clinical Trial Drugs +
1 Lasmiditan Drug Info Phase 3 Migraine [3], [4]
2 LY-334370 Drug Info Phase 2 Migraine [5], [6]
Mode of Action [+] 4 Modes of Action +
Antagonist [+] 2 Antagonist drugs +
1 Metergolin Drug Info [1]
2 1-naphthylpiperazine Drug Info [1]
Agonist [+] 10 Agonist drugs +
1 Lasmiditan Drug Info [4]
2 2-methyl-5-HT Drug Info [8]
3 5-BODMT Drug Info [9]
4 5-CT Drug Info [1]
5 alpha-methyl-5-HT Drug Info [8]
6 BRL-15572 Drug Info [10]
7 dipropyl-5-CT Drug Info [8]
8 LY344864 Drug Info [11]
9 TFMPP Drug Info [8]
10 [125I]LSD Drug Info [13]
Modulator [+] 1 Modulator drugs +
1 LY-334370 Drug Info [7]
Inhibitor [+] 1 Inhibitor drugs +
1 WAY-466 Drug Info [12]
Target Affiliated Biological Pathways
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 [+] 6 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
6 GPCRs, Other
Target-Related Models and Studies
Target Validation
Target Validation Info 
References
REF 1 Cloning 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 2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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: 3928).
REF 4 Emerging therapeutic options for acute migraine: focus on the potential of lasmiditan. Neuropsychiatr Dis Treat. 2014 Mar 31;10:547-52.
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: 20).
REF 6 G-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 7 Selective seratonin 1F (5-HT(1F)) receptor agonist LY334370 for acute migraine: a randomised controlled trial. Lancet. 2001 Oct 13;358(9289):1230-4.
REF 8 Cloning 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 9 Toward 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 10 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 11 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 12 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 13 Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. J Biol Chem. 1992 Oct 5;267(28):19761-4.

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