Ketanserin is specific 5-HT2A serotonin receptor antagonist with a
Ki of 2.5 nM for rat and human 5-HT2A. Ketanserin is a drug with
affinity for multiple G protein-coupled receptors. Ketanserin inhibits
rat and human 5-HT2C with Ki of 50 and100 nM, respectively and
has higher affinity binding for alpha-1 adrenergic (Ki = ~ 40 nM)
and Histamine H1 (Ki = 2 nM). Ketanserin can also be used to
discriminate between 5-HT1D and 5-HT1B receptor subtypes.
Ketanserin has antihypertensive properties. Ketanserin also
reduces platelet aggregation produced by serotonin. Ketanserin
also has high affinity for alpha-1 adrenergic receptors, and very
high affinity for histamine H1 receptors. Ketanserin was shown to
reduce the severity and frequency of the vasospasm in Raynaud’s
phenomenon.