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Pharmacological profile of methylphenidate-based designer drugs

Luethi, D, Kaeser, PJ, Brandt, SD, Krähenbühl, S, Hoener, MC and Liechti, ME (2017) Pharmacological profile of methylphenidate-based designer drugs. Neuropharmacology, 134 (A). pp. 133-140. ISSN 0028-3908

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Background: Methylphenidate-based designer drugs are new psychoactive substances (NPS) that are used outside medical settings and their pharmacology is largely unexplored. The aim of the present study was to characterize the pharmacology of methylphenidate-based substances in vitro. Methods: We determined the potencies of the methylphenidate-based NPS N- benzylethylphenidate, 3,4-dichloroethylphenidate, 3,4-dichloromethylphenidate, ethylnaphthidate, ethylphenidate, 4-fluoromethylphenidate, isopropylphenidate, 4- methylmethylphenidate, methylmorphenate, and propylphenidate and the potencies of the related compounds cocaine and modafinil with respect to norepinephrine, dopamine, and serotonin transporter inhibition in transporter-transfected human embryonic kidney 293 cells. We also investigated monoamine efflux and monoamine receptor and transporter binding affinities. Furthermore, we assessed the cell integrity under assay conditions. Results: All methylphenidate-based substances inhibited the norepinephrine and dopamine transporters 4 to >1,000-fold more potently than the serotonin transporter. Similar to methylphenidate and cocaine, methylphenidate-based NPS did not elicit transporter-mediated efflux of monoamines. Besides binding to monoamine transporters, several test drugs had affinity for adrenergic, serotonergic, and rat trace amine-associated receptors but not for dopaminergic or mouse trace amine-associated receptors. No cytotoxicity was observed after drug treatment at assay concentrations. Conclusion: Methylphenidate-based substances had pharmacological profiles similar to methylphenidate and cocaine. The predominant actions on dopamine transporters vs. serotonin transporters may be relevant when considering abuse liability.

Item Type: Article
Uncontrolled Keywords: 1109 Neurosciences, 1115 Pharmacology And Pharmaceutical Sciences, 1701 Psychology
Subjects: B Philosophy. Psychology. Religion > BF Psychology
Q Science > QD Chemistry
R Medicine > RM Therapeutics. Pharmacology
Divisions: Pharmacy & Biomolecular Sciences
Publisher: Elsevier
Date Deposited: 16 Aug 2017 10:55
Last Modified: 04 Sep 2021 11:18
DOI or ID number: 10.1016/j.neuropharm.2017.08.020
URI: https://researchonline.ljmu.ac.uk/id/eprint/6945
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