Atypical receptors mediate the response to endothelin-1 and SARAFOTOXIN S6B (cas 116303-65-2) in the human umbilical artery

Add time:08/02/2019    Source:sciencedirect.com

The receptors mediating smooth muscle response to endothelin-1 and SARAFOTOXIN S6B (cas 116303-65-2) in the human umbilical artery were investigated in vitro. Both agonists induced contractions that were unaffected by the endothelin ETB receptor antagonist BQ 788 (10−9, 10−8, 10−7 M). The non-selective endothelin ETA/B receptor antagonist PD 142893 (10−7 M) decreased the contraction induced by endothelin-1. PD 142893 (10-9 M) enhanced the contraction induced by sarafotoxin S6b whereas higher concentrations had no effect. Removing the endothelium did not affect the antagonising action of PD 142893 on endothelin-1-induced contractions while the enhancement of the sarafotoxin S6b-induced contraction was abolished. Sarafotoxin S6b induced relaxation in segments precontracted by 5-hydroxytryptamine and exposed to the endothelin ETA receptor antagonist BQ 123 (10−7 M) and PD 142893 (10−9 M) abolished this relaxation. These endothelial receptors seem neither to be classical endothelin ETA nor endothelin ETB receptors and they are not activated by endothelin-1.

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