High Quality Content by WIKIPEDIA articles! Ketanserin is drug with affinity for multiple G protein-coupled receptors (GPCR). Initially it was believed to be a highly selective antagonist for serotonin 5-HT2A receptors, however this not true. Ketanserin only has weak selectivity for 5-HT2A receptors over 5-HT2C receptors (~20-30 fold). Ketanserin also has high affinity for alpha-1 adrenergic receptors, and very high affinity for histamine H1 receptors. Therefore, ketanserin can not be used to reliably discriminate between the effects of 5-HT2A and 5-HT2C receptors when both are present in an experimental system. Furthermore, when alpha-1 and H1 receptors are present, the effects of ketanserin can potentially represent a complex interaction of serotonin, adrenergic, and histamine receptor systems

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