血管紧张素II受体亚型的鉴定。
Identification of angiotensin II receptor subtypes.
作者信息
Chiu A T, Herblin W F, McCall D E, Ardecky R J, Carini D J, Duncia J V, Pease L J, Wong P C, Wexler R R, Johnson A L
机构信息
Medical Products Department E. I. du Pont de Nemours & Company Wilmington, Delaware 19800-0400.
出版信息
Biochem Biophys Res Commun. 1989 Nov 30;165(1):196-203. doi: 10.1016/0006-291x(89)91054-1.
We have demonstrated the existence of two distinct subtypes of the angiotensin II receptor in the rat adrenal gland using radioligand binding and tissue section autoradiography. The identification of the subtypes was made possible by the discovery of two structurally dissimilar, nonpeptide compounds, DuP 753 and EXP655, that show reciprocal selectivity for the two subtypes. In the rat adrenal cortex, DuP 753 inhibited 80% of the total AII binding with an IC50 value on the sensitive sites of 2 x 10(-8) M, while EXP655 displaced only 20%. In the rat adrenal medulla, EXP655 gave 90% inhibition of AII binding with an IC50 value of 3.0 x 10(-8) M, while DuP 753 was essentially inactive. The combination of the two compounds completely inhibited AII binding in both tissues.
我们运用放射性配体结合法和组织切片放射自显影术，证实了大鼠肾上腺中存在两种不同亚型的血管紧张素II受体。两种结构不同的非肽类化合物DuP 753和EXP655的发现，使得这两种亚型得以鉴别，它们对两种亚型表现出相互选择性。在大鼠肾上腺皮质中，DuP 753抑制了80%的总AII结合，其在敏感位点的IC50值为2×10⁻⁸ M，而EXP655仅置换了20%。在大鼠肾上腺髓质中，EXP655对AII结合的抑制率达90%，IC50值为3.0×10⁻⁸ M，而DuP 753基本无活性。这两种化合物的组合完全抑制了两种组织中的AII结合。
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