Amfonelic acid

It was previously demonstrated that amfonelic acid, a DA-uptake blocker, partially prevented the METH-induced decrease in TPH activity (Schmidt et al. 1985). Recently, effects were investigated of a specific DA-uptake blocker, GBR 12909, on the MDMA-induced response in the serotonergic... 

Schmidt, C.J. and Gibb, J.W., Role of the dopamine uptake carrier in the neurochemical response to methamphetamine effects of amfonelic acid, Eur. J. Pharmacol., 109, 73, 1985. 

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. 

The effect of systemic administration of these amphetamine metabolites on the content of DA and its metabolites and on 5-HT was then examined. When pOHA was administered systemically (5, 15, or 30 mg/kg), the concentration of DA and its metabolites in the neostriatum was depressed. The effect on the neostriatal serotonergic system was not as pronounced as that on the dopaminergic system hippocampal serotonin content was altered only at the higher dose of pOHA and hypothalamic 5-HT concentrations were decreased at both the 15 mg and 30 mg doses. The authors then determined the effect of the monoaminergic uptake inhibitors amfonelic acid and cocaine on the response to systemically administered pOHA. The decrease in DA and its metabolites was attenuated by amfonelic acid (1 mg/kg, administered 30 minutes before pOHA), but cocaine failed to alter the effects of systemic pOHA administration. 

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