Effect of Amphetamine-Type Psychostimulants on Brain Metabolism

Recent Investigations on the Mechanism of Action of Nomifensine

“…Nomifensine is a pure catecholamine uptake blocker, whereas amphetamine and its derivatives predominantly enhance the release of catecholamines from the nerve endings [12,38,39]. The lack of any releasing activity of nomifensine has been confirmed using various in vitro models [21,39,42,43].…”

Studies on brain metabolism of biogenic amines.

“…Although nomifensine seems to share its action on the dopaminergic system with amphetamine, its mechanism of action is clearly different from that of the psychostimulant drugs. Amphetamine and its derivatives, in addition to their inhibitory activity on monoamine uptake, are acting mainly by promoting the release of catecholamines into the synaptic cleft (for refs, see Estler, 1975). The effects of nomifensine, however, on the catecholamine system, including the small increase in striatal DA turnover (Gerhards et al, 1974), are not caused by an enhancement of catecholamine release.…”

Neuroendocrine tests of monoamine function in man: a review of basic theory and its application to the study of depressive illness

“…The ACTH response to hypoglycaemia is inhibited by a-blockade with phentolamine (Nakai et al 1973), and the cortisol response to methylamphetamine is inhibited by the aantagonist, thymoxamine (Rees et al 1970). Although methylamphetamine is a strong dopamine agonist and a weak 5-HT agonist (Estler, 1975;Moore, 1977), neither dopamine nor 5-HT has important influences upon the release of ACTH in man, and so the cortisol response to methylamphetamine may depend specifically upon its effects at a-adrenoceptors. Hormonal responses to amphetamines show a clear diurnal variation (Besser et al 1969) and are inhibited by chlordiazepoxide , and for these reasons may depend upon the stimulation of central adrenoceptors.…”