Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.

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Hamblin MW, Metcalf MA

Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.

Mol Pharmacol. 1991 Aug;40(2):143-8.

PubMed ID

1652050 [ View in PubMed

]

Abstract

We describe the nucleic acid sequence encoding a human 5-hydroxytryptamine1D (5-HT1D) serotonin receptor and some of the functional characteristics of the gene product. The receptor gene was isolated by hybridization to a probe based on a canine thyroid cDNA (called RDC4) previously isolated by others and believed to encode a heretofore undetermined member of the guanine nucleotide-binding protein (G protein)-linked receptor family. The human clone we isolated, called MA6A, contains an apparently intronless open reading frame encoding a 377-amino acid polypeptide with the seven hydrophobic domains characteristic of G protein-linked receptors. The MA6A deduced amino acid sequence is 88% identical to that for RDC4 and 43% identical to that for the human 5-HT1A receptor. Expression of the human gene product in transfected cell lines results in the appearance of saturable high affinity 5-HT1D-type [3H]5-HT binding. The expressed receptor exhibits features indicative of coupling to Gi proteins, i.e., robust inhibition of forskolin-stimulated cAMP accumulation and formation of a pertussis toxin-sensitive high agonist affinity binding state. These findings may help clarify several ambiguities in the classification and action of serotonin receptor subtypes.

DrugBank Data that Cites this Article

Polypeptides

Name	UniProt ID
5-hydroxytryptamine receptor 1D	P28221	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sumatriptan	5-hydroxytryptamine receptor 1D	Ki (nM)	3.7	N/A	N/A	Details
Yohimbine	5-hydroxytryptamine receptor 1D	Ki (nM)	59	N/A	N/A	Details
Yohimbine	5-hydroxytryptamine receptor 1D	Ki (nM)	51	N/A	N/A	Details