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Pharmacological Characterization of 4-Methylthioamphetamine Derivatives

Laboratorio de Neuroquímica y Neurofarmacología, Centro de Neurobiología y Fisiopatología Integrativa (CENFI), Instituto de Fisiología, Facultad de Ciencias, Universidad de Valparaíso, Valparaíso 2360102, Chile
Center for Bioinformatics, Simulations and Modelling, University of Talca, Talca 3460000, Chile
Laboratorio de Síntesis Orgánica y Farmacología Molecular, Departamento de Ciencias Químicas y Recursos Naturales, Facultad de Ingeniería y Ciencias, Universidad de la Frontera, Temuco 4811230, Chile
Center of Excellence in Biotechnology Research Applied to the Environment, Universidad de La Frontera, Temuco 4811230, Chile
Department of Neurobiology and Anatomy, Drexel University College of Medicine, Philadelphia, PA 19129, USA
Centro de Investigación Biomédica y Aplicada (CIBAP), Escuela de Medicina, Facultad de Ciencias Médicas, Universidad de Santiago de Chile, Santiago 9170022, Chile
Facultad de Ciencias de la Salud, Universidad Autónoma de Chile, Talca 3467987, Chile
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Tomasz Plech, Marta Andres-Mach and Diego Muñoz-Torrero
Molecules 2020, 25(22), 5310;
Received: 15 September 2020 / Revised: 30 October 2020 / Accepted: 11 November 2020 / Published: 13 November 2020
Amphetamine derivatives have been used in a wide variety of pathologies because of their pharmacological properties as psychostimulants, entactogens, anorectics, and antidepressants. However, adverse cardiovascular effects (sympathomimetics) and substance abuse problems (psychotropic and hallucinogenic effects) have limited their use. 4-Methylthioamphetamine (MTA) is an amphetamine derivative that has shown to inhibit monoamine uptake and monoamine oxidase. However, the pharmacological characterization (neurochemical, behavioral, and safety) of its derivatives 4-ethylthioamphetamine (ETA) and 4-methylthio-phenil-2-butanamine (MT-But) have not been studied. In the current experiments, we show that ETA and MT-But do not increase locomotor activity and conditioned place preference with respect to MTA. At the neurochemical level, ETA and MT-But do not increase in vivo DA release in striatum, but ETA and MT-But affect the nucleus accumbens bioaccumulation of DA and DOPAC. Regarding cardiovascular effects, the administration of MTA and ETA increased the mean arterial pressure and only ETA significantly increases the heart rate. Our results show that the pharmacological and safety profiles of MTA are modulated by changing the methyl-thio group or the methyl group of the aminoethyl chain. View Full-Text
Keywords: conditioned place preference (CPP); DAT; locomotor activity; reward; FSCV; molecular docking conditioned place preference (CPP); DAT; locomotor activity; reward; FSCV; molecular docking
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MDPI and ACS Style

Guajardo, F.G.; Velásquez, V.B.; Raby, D.; Núñez-Vivanco, G.; Iturriaga-Vásquez, P.; España, R.A.; Reyes-Parada, M.; Sotomayor-Zárate, R. Pharmacological Characterization of 4-Methylthioamphetamine Derivatives. Molecules 2020, 25, 5310.

AMA Style

Guajardo FG, Velásquez VB, Raby D, Núñez-Vivanco G, Iturriaga-Vásquez P, España RA, Reyes-Parada M, Sotomayor-Zárate R. Pharmacological Characterization of 4-Methylthioamphetamine Derivatives. Molecules. 2020; 25(22):5310.

Chicago/Turabian Style

Guajardo, Fabrizzio G., Victoria B. Velásquez, Daniela Raby, Gabriel Núñez-Vivanco, Patricio Iturriaga-Vásquez, Rodrigo A. España, Miguel Reyes-Parada, and Ramón Sotomayor-Zárate. 2020. "Pharmacological Characterization of 4-Methylthioamphetamine Derivatives" Molecules 25, no. 22: 5310.

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