Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
Article Details
- CitationCopy to clipboard
Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA
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.
- PubMed ID
- 8380639 [ View in PubMed]
- Abstract
An intronless gene encoding an additional human serotonin (5-HT) 5-HT1-like receptor subtype was isolated from a human genomic library with probes obtained from degenerate PCR primers used to amplify 5-HT-receptor-specific sequences. The highest degree of homology was found with the 5-HT1E subtype (70%) and the 5-HT1D alpha (63%) and 5-HT1D beta (60%) receptors. RNA for this gene was detected in the human brain but was not detected in kidney, liver, spleen, heart, pancreas, and testes. High-affinity (Kd = 9.2 nM) 3H-labeled 5-HT binding was detected. Competition studies revealed the following rank order of potencies for serotonergic ligands: 5-HT > sumatriptan >> 5-carboxyamidotryptamine > 8-hydroxy-2(di-1-propylamino)tetralin > spiperone. 5-HT produced a dose-dependent inhibition of forskolin-stimulated cAMP accumulation (EC50 = 7.9 nM) in transfected cells. These properties distinguish this receptor from any previously characterized and establish a fifth 5-HT1-like receptor subtype (5-HT1F) coupled to the inhibition of adenylate cyclase.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Methysergide 5-hydroxytryptamine receptor 1E Protein Humans UnknownBinderDetails Methysergide 5-hydroxytryptamine receptor 1F Protein Humans UnknownBinderDetails - Polypeptides
Name UniProt ID 5-hydroxytryptamine receptor 1F P30939 Details - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Ergotamine 5-hydroxytryptamine receptor 1F Ki (nM) 171 N/A N/A Details Methysergide 5-hydroxytryptamine receptor 1F Ki (nM) 34 N/A N/A Details Sumatriptan 5-hydroxytryptamine receptor 1F Ki (nM) 23 N/A N/A Details