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(Paper) monoamine releasing properties of designer drugs

V

vecktor

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Jan 17, 2006
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this paper on the releasing and reuptake properties of designer drugs bought in tokyo adult shops, is quite interesting because it is the only place I have seen the IC50's for DA NE SE for MBDB Methylone BDB and 4-F AMP in the same place with the same technique. in fact almost all the common ones are there including some piperazines.
I noticed that MDMA in this assay is equipotent at releasing NE and SE but about 5 time worse at dopamine. which is interesting because it has always been assumed that MDMA is primarily a DA SE releaser. this is a rat study though
it is also interesting that MCPP is a potent releaser of serotonin, so I suppose the crappy effects of this particularly crappy piperazine comes from its action as a 5ht2c agonist ( though possibly that is the mechanism by which it is releasing serotonin)
worth a read and a think.
I cannot post the paper, perhaps someone who can might like to
V

Abstract

Eur J Pharmacol. 2006 Dec 12; : 17223101

The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain.
[My paper] Fumiko Nagai , Ryouichi Nonaka , Kanako Satoh Hisashi Kamimura

We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BDB), and N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine. 4-Fluoroamphetamine, methylone and BDB also strongly increased the release of the three monoamines, but MBDB increased 5-HT and norepinephrine release, but had little effect on dopamine release. However, 2,5-dimethoxy-4-iodophenethylamine (2C-I), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,4,5-trimethoxyamphetamine (TMA-2) and 2,4,6-trimethoxyamphetamine (TMA-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. alpha-Metyltryptamine (AMT), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. The tryptamine derivative, 5-methoxy-alpha-methyltryptamine (5-MeO-AMT), also strongly inhibited re-uptake and increased the release of the three monoamines. N,N-dipropyltryptamine (DPT), 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT), 5-methoxy-N,N-methylisopropyltryptamine (5-MeO-MIPT), and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-Chlorophenyl)piperazine (3CPP) and 1-(methoxyphenyl)piperazine (4MPP), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. The results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs.
Click to expand...
 
I really don't know. there has been a lot of pressure to make them illegal. and I suspect they probably fell into some kind of grey area rather than being explicitly legal or illegal, the only info I have is that at the turn of this year 06/07 they were still legal.
V
 
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