Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes.
Biochem Biophys Res Commun
; 175(2): 556-61, 1991 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-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.
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Base de dados:
MEDLINE
Assunto principal:
Venenos de Víboras
/
Endotelinas
/
Receptores de Superfície Celular
Limite:
Animals
Idioma:
En
Ano de publicação:
1991
Tipo de documento:
Article