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Home , Phenethylamine

P.1.g.036 and interaction profiles of novel derivatives Dino Luethi1, Philine J Kaeser1, Anna Rickli1, Marius C Hoener2, Matthias E Liechti1

1Clinical Pharmacology and Toxicology, University Hospital Basel, Basel, Switzerland 2Neuroscience Research, F. Hoffmann-La Roche Ltd, Basel, Switzerland

Introduction Methods Novel psychoactive constantly emerge on the illicit HEK cells overexpressing human - (hSERT) - drug market and are often sold as “legal highs” over the Internet as (hDAT), or - (hNET) re-uptake transporters were used alternatives to illegal drugs. In the current study, we investigated the in for uptake and release experiments. To determine the potency of drugs 3 vitro pharmacological mechanism of action of the novel phenethylamine to inhibit monoamine-uptake, we assessed uptake of [ H]-labelled monoamines in presence of different drug concentrations. For the derivatives 5-(2-aminopropyl)indole (5-IT), 3,4- release assay, we pre-loaded the cells with the respective [3H]- dimethylmethcathinone (3,4-DMMC), 4-methylamphetamine (4-MA), 3- monoamines, washed, and induced release with the addition of the methylmethcathinone (3-MMC), and N-methyl-2-aminoindane (N- drugs at a single high concentration. methyl-2-AI).

Figure 1. Structures of novel phenethylamine derivatives. Results

Figure 2. Monoamine transporter inhibition. Figure 3. Drug induced monoamine release.

Conclusion The authors report no conflict of interest. All substances strongly inhibited the NET as it is known for classic , suggesting Contact: [email protected] marked sympathomimetic properties. 3,4-DMMC and 4-MA inhibited the SERT more strongly [email protected] than the DAT, thereby exhibiting pharmacological properties similar to 3,4- methylenedioxymethamphetamine (MDMA) and suggesting similar empathogenic effects. All substances were releasers of monoamines. However, 5-IT caused efflux of DA and 5-HT but not NE and N-methyl-2-AI caused efflux of NE only.