Review
5-HT2 receptor subtypes: A family re-united?

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Abstract

The current classification for 5-HT2 receptors accommodates three subtypes. In addition to the originally defined 5-HT2 receptor, sanctuary is now provided for the structurally related 5-HT1C receptor (now 5-HT2C) and at least one atypical 5-HT receptor subtype. The strong functional union of this family is reflected in the paucity of ligands that will discriminate between its subtypes and prompts some re-evaluation of the activities of compounds which may now be regarded as nonselective for the receptor subtypes in this class. In this article, Gordon Baxter and colleagues examine the pharmacology of both officially recognized and atypical 5-HT2 receptor subtypes. A number of novel selective agents are highlighted, some of which may prove useful for 5-HT2 receptor classification and, ultimately, clarify the mechanistic basis for current and future therapeutic strategies which target this receptor family.

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    Citation Excerpt :

    Tanaka and colleagues, by functional and immunohistochemical studies, also characterized 5-HT2A and 5-HT1B receptors in smooth muscle cells of this vessel (Tanaka et al., 2008). The now observed contractile effect of MDMA, in the human internal mammary artery, is in accordance with the above described findings since ketanserin, a selective 5-HT2A/2C antagonist (pKi of 8.9 and 7.0 at 5-HT2A and 5-HT2C receptors) (Baxter et al., 1995) altered both MDMA and 5-HT concentration-response curves, almost abolishing the 5-HT maximum contraction, making the 5-HT-induced contractile effect in this vessel almost mediated by this subtype receptor, similarly to what was reported on other peripheral non intracranial blood vessels, namely the human uterine artery (Karlsson et al., 1997). An antagonism at 5-HT2C receptors is most unlikely, since they have not yet been described in the cardiovascular system (Hoyer et al., 1994; Watts and Davis, 2011).

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