Ketanserin (5-HT2A serotonin receptor antagonist) - 50 mg

Ketanserin, known also as Vulketan Gel, is a specific 5-HT2A serotonin receptor antagonist. It can also be used to discriminate between 5-HT1D and 5-HT1B receptor subtypes.

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.