5-HT1 receptors

Overview

The 5-HT1 receptor family comprises five different receptors (5-HT1A, 5-HT1B, 5-HT1D, 5-ht1e, 5-HT1F), which share 40-63% amino acid sequence identity and can couple to Gi/Go to inhibit cAMP formation, although... [read more] signaling via other transduction systems are known (e.g. 5-HT1A receptor activates G-protein-gated inwardly rectifying K+ channel [GIRK]). One of the 5-HT1 receptor class, the 5-ht1e receptor, is yet to achieve receptor status since a robust response mediated via the protein is yet to be reported in the literature; lower-case appellation is used to denote this. 5-HT1A and 5-HT1B receptors act as somatodendritic and terminal autoreceptors, respectively; however, these receptors are also expressed throughout the CNS.PharmacologyA number of well-defined selective agonists (e.g. 8-OH-DPAT [5-HT1A receptor], PNU 109291 [5-HT1D receptor], LY 344864 [5-HT1F receptor]) and antagonists (e.g. WAY100635 [5-HT1A receptor], SB236057 [5-HT1B receptor], SB714786 [5-HT1D receptor]), are available to selectively probe some individual members of the 5-HT1 receptors.Clinical significance5-HT1A receptors are targeted by the anxiolytic drug, buspirone, which is a partial agonist. Various ‘triptans’ (e.g. sumitriptan and zolmitriptan) are used to treat acute migraine attack, these drugs are 5-HT1B/5-HT1D receptor agonists, with some also having agonist activity at the 5-HT1F receptor. [close]