Photoaffinity labeling of human platelet and rabbit kidney α2
-adrenoceptors with [3
A newly developed α2-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 ∼ 80 Ci/mmol. Using membranes prepared from human platelets and from rabbit kidney, α2-adrenoceptors have been covalently labeled following photolysis in the presence of [3H]SKF 102229. As determined by SDS-PAGE, the apparent molecular weight of α2-adrenoceptors from both of these tissues was 64,000. The yield of covalent insertion of [3H]SKF 102229 into the α2-adrenoceptor was very good. Thus, following photolysis up to 90% of the α2-adrenoceptors could be irreversibly labeled with [3H]SKF 102229. © 1986.
Regan, JW; Raymond, JR; Lefkowitz, RJ; DeMarinis, RM
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