Nomifensine dopamine transporter

Dopamine is removed from the synapse via two mechanisms. First, COMT degrades intrasynaptic DA. Second, the dopamine transporter (DAT) [see (4) in Fig. 2.9], a Na /CD-dependent neurotransmitter transporter, transports DA in either direction, depending on the concentration gradient. The DAT is blocked selectively by drugs such as cocaine, amphetamine, bupropion, and nomifensine. 

The dopamine uptake system - or dopamine transporter system - is inhibited by the following clinically used agents amfonelic acid, bupropion, mazindot or experimental agents, nomifensine, indatraline, p-CFT, p-ClT-FP, GYKl 52895 and LR 5182. 

Raitiri, M. Cerrito, F. Cervoni, A.M. and Levi, G. Dopamine can be released by two mechanisms differentially affected by the dopamine transport inhibitor nomifensine. J Pharmacol Exp Ther 208 195-202, 1979. 

Nomifensine is a substituted phenyipiperidine (an aminophenyitetrahydroisoquinoline) structurally related to sertraline that was marketed as a stimulatory antidepressant in the mid-1970s but later withdrawn because of a high incidence of hemolytic anemia. Nomifensine inhibits the NE and dopamine reuptake transporters. It displays high affinity for NET (human pK, = 7.8), moderate affinity for dopamine transporter (pK, = 6.6), and a low affinity for SERT (5-HT NE ratio, 65). 

---