The selective accumulation of bretylium in sympathetic ganglia and their postganglionic nerves

A study of the distribution of [(14)C]-labelled bretylium (N-o-bromobenzyl-N-ethyl-N,N-dimethylammonium) in cat tissues at various times after subcutaneous injection suggests that the specificity of its blocking action on adrenergic neurones may be related to its selective accumulation in these neurones. The rate of rise and fall of concentration in sympathetic ganglia and postganglionic sympathetic nerves showed a close similarity to the time course of the blocking adrenergic neurones as manifested by relaxation of the nictitating membranes. Concentrations found were similar to those in adrenergic nerve trunks when topical application of the drug had caused a local block of conduction. Conduction in other types of nerve could be blocked by topical application, but in general they were less sensitive, heavily myelinated nerves being the most resistant.