The reactions of 2-halogenoethylamines at the noradrenaline receptor-storage complex

The alkylation reactions of 2-halogenoethylamines are briefly reviewed. The rates of recovery of aortic strips following exposure to 2-halogenoethylamines have been determined and arguments are presented which suggest that the anionic site of the α-receptor, complementary to the ammonium function of noradrenaline, may be best represented by a carboxylate anion. Some evidence is presented which indicates the presence of a second nucleophilic site in close proximity to the carboxylate anion. The irreversible actions of 2-halogenoethylamines at the noradrenaline storage site(s) are discussed. It is suggested that alkylation of a non-regeneratable nucleophilic group is involved in the inactivation of noradrenaline storage mechanisms.