PMID: 19912901Dec 1, 1992Paper

Distinct 5-HT(1B) and 5-HT(1D) serotonin receptors in rat: Structural and pharmacological comparison of the two cloned receptors

Molecular and Cellular Neurosciences
M W HamblinK M Merchant

Abstract

We and others have recently cloned the genes encoding the human 5-HT(1D) (5-HT(1Dalpha)) and 5-HT(1B) (5-HT(1Dbeta)) serotonin receptors. Because of the history of profound species differences in the pharmacology of these receptor subtypes, we also cloned the homologous genes for these two receptors in rat. The rat 5-HT(1D) receptor gene, like that of the rat 5-HT(1B) receptor, is intronless, encoding a 374-amino acid polypeptide 90% identical to its human homologue. The rat 5-HT(1D) and rat 5-HT(1B) receptors are 61% identical in their deduced amino acid sequences. The availability of both the rat 5-HT(1B) and 5-HT(1D) genes allowed direct comparison of the pharmacological properties of the two receptors expressed in transfected cells as assessed using 5-[(3)H]HT binding assays. Unlike the rat 5-HT(1B) receptor, which is pharmacologically dimorphic with respect to its human homologue, the rat 5-HT(1D) receptor has an almost identical profile compared to the human 5-HT(1D) receptor. (+/-)-Cyanopindolol and (-)-propranolol are more than 100-fold selective for the rat 5-HT(1B) receptor over the rat 5-HT(1D) receptor, while mianserin is more than 100-fold selective for the rat 5-HT(1D) receptor. The rat 5-HT(1D) receptor is expres...Continue Reading

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Jun 1, 1993·Naunyn-Schmiedeberg's Archives of Pharmacology·A T BruinvelsD Hoyer
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