用[3H]SKF 102229对人血小板和兔肾α2-肾上腺素能受体进行光亲和标记。

Photoaffinity labeling of human platelet and rabbit kidney alpha 2-adrenoceptors with [3H]SKF 102229.

作者信息

Regan J W, Raymond J R, Lefkowitz R J, DeMarinis R M

出版信息

Biochem Biophys Res Commun. 1986 Jun 13;137(2):606-13. doi: 10.1016/0006-291x(86)91121-6.

Abstract

A newly developed alpha 2-adrenergic photoaffinity ligand, 3-methyl-6-chloro-9-azido-1H-2,3,4,5-tetrahydro-3-benzazepine (SKF 102229), has been radiolabeled with tritium to a specific activity of approximately 80 Ci/mmol. Using membranes prepared from human platelets and from rabbit kidney, alpha 2-adrenoceptors have been covalently labeled following photolysis in the presence of [3H]SKF 102229. As determined by SDS-PAGE, the apparent molecular weight of alpha 2-adrenoceptors from both of these tissues was 64,000. The yield of covalent insertion of [3H]SKF 102229 into the alpha 2-adrenoceptor was very good. Thus, following photolysis up to 90% of the alpha 2-adrenoceptors could be irreversibly labeled with [3H]SKF 102229.

摘要

一种新开发的α2 - 肾上腺素能光亲和配体，3 - 甲基 - 6 - 氯 - 9 - 叠氮基 - 1H - 2,3,4,5 - 四氢 - 3 - 苯并氮杂卓（SKF 102229），已用氚进行放射性标记，比活度约为80 Ci/mmol。使用从人血小板和兔肾制备的膜，在[3H]SKF 102229存在下光解后，α2 - 肾上腺素能受体已被共价标记。通过SDS - PAGE测定，这两种组织的α2 - 肾上腺素能受体的表观分子量为64,000。[3H]SKF 102229共价插入α2 - 肾上腺素能受体的产率非常高。因此，光解后高达90%的α2 - 肾上腺素能受体可以被[3H]SKF 102229不可逆地标记。