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Sarafotoxin S6c: An Agonist Which Distinguishes Between Endothelin Receptor Subtypes

D L Williams Jr, K L Jones, D J Pettibone, E V Lis, B V Clineschmidt

Biochem Biophys Res Commun. 1991 Mar 15;175(2):556-61.

PMID: 1850245

Abstract:

In contrast to endothelin-1 (ET-1) and several of its analogues, sarafotoxin S6c (S6c) was a much more potent inhibitor of [125I]-ET-1 binding in rat hippocampus and cerebellum (Ki approximately 20 pM) than in rat atria and aorta (Ki approximately 4500 nM), suggesting the existence of ET-1 receptor subtypes (aorta/atria, ETA; hippocampus/cerebellum, ETB). S6c was a potent activator of PI turnover in hippocampus (EC50 approximately 10 nM) but not atria (EC50 greater than 1 microM), unlike ET-1 which was active in both tissues. S6c, therefore, is a highly selective ETB agonist. Furthermore, S6c was a potent pressor agent in the pithed rat (ED25 mm Hg approximately 0.1 nmoles/kg, i.v.), suggesting that the ETB receptor subtype may be important in cardiovascular function.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP121695872 Sarafotoxin S6c Sarafotoxin S6c 121695-87-2 Price
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