<i>In Vitro</i> Screening of Psychoactive Drugs to Prevent the Abuses

Abstract

The Tokyo Metropolitan Government in Japan enacted an "Ordinance concerning the abuse prevention of the psychoactive drugs" in April 2006 that prohibited the manufacture, cultivation, sales, possession, use, etc., of these drugs. Therefore, we constructed a reproducible, simple, and small-scale determination method of the psychoactive drugs for the re-uptake and the release of monoamines (dopamine, serotonin and norepinephrine), and the activation of [(35)S]guanosine-5'-O-(3-thio)-triphosphate binding to guanine nucleotide-binding proteins (G proteins). These assays were then applied to study the effects of different kinds (phenethylamine derivatives, tryptamine derivatives, and piperazine derivatives) of non-medically used psychoactive drugs on monoamine re-uptake and release, and G-protein binding. The results suggested that some drugs strongly act on the central nerve system to the same extent as the drugs. This assay system was able to designate psychoactive drugs as prohibited substances in accordance with criteria set forth by the Tokyo Metropolitan government.