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  • Title: Subtypes of endothelin ETA and ETB receptors mediating venous smooth muscle contraction.
    Author: Sudjarwo SA, Hori M, Tanaka T, Matsuda Y, Okada T, Karaki H.
    Journal: Biochem Biophys Res Commun; 1994 Apr 15; 200(1):627-33. PubMed ID: 8166738.
    Abstract:
    In rabbit saphenous vein, endothelin (ET)-1 and ET-3 induced sustained contractions whereas the selective agonists of the ETB receptor, sarafotoxin S6c (STXc) and IRL 1620, induced transient contractions. In the presence of an ETA antagonist, BQ-123, contractions induced by ET-1, STXc and IRL 1620 did not change whereas ET-3 induced only transient contraction. The ETB antagonists, RES-701-1 and IRL 1038, only weakly antagonized the effects of these stimulants. In the muscle pretreated with STXc, neither STXc nor IRL 1620 was effective whereas ET-3 induced sustained contraction at higher concentrations than ET-1. In the muscle pretreated with STXc, BQ-123 weakly antagonized the effect of ET-1 and abolished the effect of ET-3. These results suggest that there are two types of ET receptors; less tachyphylactic and isopeptide-selective ETA receptor, and tachyphylactic and isopeptide-nonselective ETB receptor. The ETA receptors may be further classified as a BQ-123-sensitive ETA1 and a BQ-123-insensitive ETA2 subtypes. The ETB receptors may also be subclassified as the ETB1 and ETB2 subtypes based on the sensitivity to the ETB antagonists.
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