Definitions for ketanserin
This page provides all possible meanings and translations of the word ketanserin
A serotonin antagonist.
Ketanserin is a drug with affinity for multiple G protein-coupled receptors. It is a highly selective antagonist for serotonin 5-HT2A receptors, but also has moderate selectivity for 5-HT2C receptors and 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. Complicating the matter further is the fact that ketanserin has moderate affinity for delta-1t adrenergic receptor and 5-HT6 receptors as well as weak affinity for dopamine D1 and D2 receptors. Ketanserin at levels of 500 nM or greater are thus potentially affecting at least 8 different GPCRs from 4 different families. Receptors for which ketanserin has high affinity binding: ⁕5-HT2A = 2-3 nM
U.S. National Library of Medicine
A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
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