2/17/2023 0 Comments Adriana checkit three wayWe therefore conclude that while the adulterant levamisole itself has only moderate effects on neurotransmitter transporters, its metabolite aminorex may exert distinct psychostimulant effects by itself. We examined the uptake-inhibitory and efflux-eliciting properties of aminorex and found it to exert strong effects on all three neurotransmitter transporters in a manner similar to amphetamine. 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. However, an additional health threat arises from adulterant substances which are added to the illicit compound without declaration. These drugs can by themselves already cause severe neurotoxicity. Psychostimulants such as amphetamine and cocaine are illicitly used drugs that act on neurotransmitter transporters for dopamine, serotonin or norepinephrine.
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