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Drug intelligence / Profile preview
ketanserin
- Development stage
- Phase 4
- Lead developer
- Johnson & Johnson
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Topical
01
Overview
Ketanserin is an antihypertensive agent primarily used to treat arterial hypertension and vasospastic disorders. It acts as a high-affinity, non-selective antagonist of serotonin 5-HT2 receptors (notably 5-HT2A) and also exhibits antagonistic activity at histamine H1 receptors and weak alpha 1-adrenoceptor blocking properties. Ketanserin inhibits serotonin-induced vasoconstriction, platelet activation, and aggregation, leading to reduced systemic vascular resistance and improved vascular compliance. It has been shown to lower blood pressure—especially in older adults—and improve microcirculation in conditions such as Raynaud's disease and scleroderma-related ulcers. Ketanserin is also used in scientific research for its antiserotonergic effects on the serotonin system[1][3][4][5][8].
- Brand names
- Sufrexal
- Other names
- ketanserina
02
Targets
HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)ADRA1A (α1A)HRH1 (Histamine H1 Receptor)
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