5-HT7 receptor

Overview

The 5-HT7 receptor is a GPCR that couples via Gs to increase cAMP production with some other transduction pathways also implicated in receptor function (e.g. ERK, Galpha12/RhoA/Cdc42). The structure displays less than 39% amino acid sequence identity to other 5-HT receptors. Several splice variants have been described.PharmacologyVarious selective 5-HT7 receptor agonists (e.g. LP-12, AS-19 [partial agonist]) and antagonists (e.g. SB 269970, SB656104-A) have been described.Clinical significanceSimilar to the 5-HT6 receptor, various non-selective psychotropic drugs also display high affinity for the 5-HT7 receptor (e.g. asenapine, clozapine, pimozide), although the consequences of this interaction are also not clear.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Human non-orphan GPCRs
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Reference agonist:
serotonin
EC50:
1.8 nM
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Mouse non-orphan GPCRs
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Reference agonist:
serotonin
EC50:
55 nM