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 | |||||
| Sequence |
MDFLNSSDQNLTSEELLNRMPSKILVSLTLSGLALMTTTINSLVIAAIIVTRKLHHPANY
LICSLAVTDFLVAVLVMPFSIVYIVRESWIMGQVVCDIWLSVDITCCTCSILHLSAIALD RYRAITDAVEYARKRTPKHAGIMITIVWIISVFISMPPLFWRHQGTSRDDECIIKHDHIV STIYSTFGAFYIPLALILILYYKIYRAAKTLYHKRQASRIAKEEVNGQVLLESGEKSTKS VSTSYVLEKSLSDPSTDFDKIHSTVRSLRSEFKHEKSWRRQKISGTRERKAATTLGLILG AFVICWLPFFVKELVVNVCDKCKISEEMSNFLAWLGYLNSLINPLIYTIFNEDFKKAFQK LVRCRC |
||||
| Drugs and Mode of Action | |||||
| Drug(s) | Lasmiditan | Drug Info | Phase 3 | Migraine | [1], [2] |
| LY-334370 | Drug Info | Phase 2 | Migraine | [3], [4] | |
| Antagonist | 1-naphthylpiperazine | Drug Info | [5] | ||
| metergoline | Drug Info | [5] | |||
| Agonist | 2-methyl-5-HT | Drug Info | [6] | ||
| 5-BODMT | Drug Info | [7] | |||
| 5-CT | Drug Info | [5] | |||
| alpha-methyl-5-HT | Drug Info | [6] | |||
| BRL-15572 | Drug Info | [8] | |||
| dipropyl-5-CT | Drug Info | [6] | |||
| Lasmiditan | Drug Info | [1] | |||
| LY344864 | Drug Info | [9] | |||
| TFMPP | Drug Info | [6] | |||
| [125I]LSD | Drug Info | [10] | |||
| Modulator | LY-334370 | Drug Info | |||
| Inhibitor | WAY-466 | Drug Info | [11] | ||
| 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 1 | Emerging therapeutic options for acute migraine: focus on the potential of lasmiditan. Neuropsychiatr Dis Treat. 2014 Mar 31;10:547-52. | ||||
| REF 2 | (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 3 | 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 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: 20). | ||||
| REF 5 | 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 6 | 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 7 | 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 8 | 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 9 | 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 10 | Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. J Biol Chem. 1992 Oct 5;267(28):19761-4. | ||||
| REF 11 | J 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. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.