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Nonaka R, Nagai F, Ogata A, Satoh K.
“In vitro screening of psychoactive drugs by [(35)S]GTPgammaS binding in rat brain membranes”.
Biol Pharm Bull. 2007 Dec 06;30(12):2328-33.
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Abstract
We constructed a reproducible, simple, and small-scale determination method of the psychoactive drugs that acted directly on the monoamine receptor by measuring the activation of [(35)S]guanosine-5'-O-(3-thio)-triphosphate binding to guanine nucleotide-binding proteins (G proteins). This method can simultaneously measure the effects of three monoamines, namely dopamine (DA), serotonin (5-HT), and norepinephrine (NE), in rat brain membranes using a 96-well microplate. Activation of D(1) and D(2) receptors in striatal membranes by DA as well as 5-HT and NEalpha(2) receptors in cortical membranes could be measured. Of 12 tested phenethylamines, 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), and 2,5-dimethoxy-4-iodophenethylamine (2C-I) stimulated G protein binding. The other phenethylamines did not affect G protein binding. All 7 tryptamines tested stimulated G protein binding with the following rank order of potency; 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT)gt;;5-methoxy-N,N-diallyltryptamine (5-MeO-DALT)gt;;5-methoxy-alpha-methyltryptamine (5-MeO-AMT)gt;;or=5-methoxy-N,N-methylisopropyltryptamine (5-MeO-MIPT)gt;;5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT)gt;;N,N-dipropyltryptamine (DPT)gt;;or=alpha-methyltryptamine (AMT). This assay system was able to designate psychoactive drugs as prohibited substances in accordance with criteria set forth by the Tokyo Metropolitan government.
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