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Levamisole is metabolized to aminorex, a formerly marketed anorectic drug, which is classified as an amphetamine-like substance. Because levamisole and cocaine are frequently co-administered, we searched for possible allosteric effects at 30 μM, a concentration at which levamisole displayed already mild effects on norepinephrine transport it did not enhance the inhibitory action of cocaine.

In addition, levamisole did not trigger any appreciable substrate efflux. Levamisole was 100 and 300-fold less potent than cocaine in blocking norepinephrine and dopamine uptake, and had only very low affinity for the serotonin transporter. We tested the effects of levamisole on neurotransmitter transporters heterologously expressed in HEK293 cells.

One of the most frequently added adulterants in street drugs sold as cocaine is the anthelmintic drug levamisole.

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