N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)pyridin-4-yl]pyrimidin-4-yl]-5-methyl-pyridine-2-sulfonamide

Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction[1][5].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor

Clazosentan (0.1 μM) inhibits the ETA receptor in cerebral arteries[3]. Clazosentan is a substrate of the organic anion-transporting polypeptide (OATP) 1B1/1B3[5].

Clazosentan (10 μM, 0.05 mL/kg, intracisternal injection) inhibits the contractile responses to ET-1 in rats[2]. Clazosentan (10 mg/kg, s.c.) inhibits IL-33-induced hypernociception in mice[4]. Animal Model: Rats[2] Dosage: 10 μM, 0.05 mL/kg Administration: Intracisternal injection Result: Inhibited the contractile responses to ET-1, without preventing SAH-induced upregulation of ET receptors in cerebral arteries.