Endothelin ET(B1) receptor-mediated relaxation of rabbit basilar artery

This study tests whether endothelin receptor agonist-induced relaxation of the cerebral vasculature is mediated via endothelin ET(B1) receptor activation. Sarafotoxin S6c, an endothelin ET(B) receptor agonist, relaxed rabbit basilar artery constricted with serotonin in situ. BQ788 (N-cis-2,6-dimethylpiperidinocarbonyl L-gamma-MeLeu-D-Trp (COOCH3)-Nle), and RES-701-1 (Gly-Asn-Trp-His-Gly-Thr-Ala-Pro-Asp-Trp-Phe-Phe-Asn-Tyr-Tyr-Trp), endothelin ET(B1/B2) and endothelin ET(B1) receptor antagonists, respectively, prevented sarafotoxin S6c-induced relaxation. RES-701-1 was selective for the ET(B1) receptor, as the endothelin-1 constriction elicited in the presence of BQ610 (homopiperidenyl-CO-Leu-D-Trp (CHO)-D-Trp-OH), an endothelin ET(A) receptor antagonist, was enhanced by RES-701-1, and relaxed by BQ788. These results represent the first demonstration of the presence of endothelin ET(B1) receptors in the cerebral vasculature.