Powerful Adrenergic Neurone-blocking Agents related to Choline 2,6-Xylyl Ether Bromide

Abstract

THE discovery that the functioning of the post-ganglionic sympathetic adrenergic nerves could be impaired by choline 2,6-xylyl ether bromide (I), TM 10 (refs. l, 2), led to a search for compounds having a similar effect, but lacking the parasympathomimetic actions which preclude its use in man³. Such a selective blocking action was found in a series of benzyl quaternary ammonium salts⁴, and one of these, bretylium tosylate, was eventually shown to be a valuable antihypertensive agent in man⁵. This compound can depress conduction in various nerves, and the specificity of its blocking effect on the sympathetic nervous system seems to be related to its selective accumulation in adrenergic neurones (unpublished work).