Three apparent receptor subtypes for the endothelin/sarafotoxin family

• Published in: FEBS letters Vol. 253; no. 1; pp. 199 - 202
• Main Authors: Kloog, Y., Bousso-Mittler, D., Bdolah, A., Sokolovsky, M.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 14.08.1989; Elsevier
• Subjects: Animals; aorta; Aorta - metabolism; Binding, Competitive; Biological and medical sciences; Caudate Nucleus - metabolism; Cell receptors; Cell structures and functions; Cerebellum - metabolism; E-Sα, a high-affinity ET-1/SRTX-b subtype; E-Sβ, a high-affinity SRTX-c subtype; E-Sγ, subtype that binds all of the peptides under investigation with high affinity; Endothelin; Endothelins; ET, endothelin; Fundamental and applied biological sciences. Psychology; heart; Heart Atria - metabolism; In Vitro Techniques; Miscellaneous; Molecular and cellular biology; Peptides - metabolism; Rat, Brain, Aorta, Heart, Uterus; Rats; Receptor subtype; Receptors, Cell Surface - classification; Receptors, Cell Surface - metabolism; Receptors, Endothelin; Sarafotoxin; SRTX, sarafotoxin; uterus; Viper Venoms - metabolism; E-S β, a high-affinity SRTX-c subtype; Endothelin; E-S γ, subtype that binds all of the peptides under investigation with high affinity; Receptor subtype; E-S α, a high-affinity ET-1/SRTX-b subtype; Sarafotoxin; ET, endothelin; Rat, Brain, Aorta, Heart, Uterus; SRTX, sarafotoxin; Molecular form; Biological receptor
• ISSN: 0014-5793; 1873-3468
• DOI: 10.1016/0014-5793(89)80958-5

Competition binding experiments performed with 125I-sarafotoxin (SRTX)-b and SRTX-b, SRTX-c and endothelin (ET-1 and ET-3) using homogenates of rat right and left atria, aorta, uterus, cerebellum and caudate putamen indicated heterogeneity of the ET/SRTX receptor. The evidence pointed to the existence of three receptor subtypes: a high-affinity ET-1/SRTX-b subtype typical of smooth muscle (E-S α receptor), a high-affinity SRTX-c subtype typical of the cerebellum (E-S β receptor), and a less selective subtype typical of the caudate putamen that binds all of these peptides with high affinity (E-S γ receptor).