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Electrophysiological Actions of Synthetic Cathinones on Monoamine Transporters.
Curr Top Behav Neurosci. 2017; 32:73-92.CT

Abstract

Products containing psychoactive synthetic cathinones, such as mephedrone and 3,4-methylenedioxypyrovalerone (MDPV) are prevalent in our society. Synthetic cathinones are structurally similar to methamphetamine, and numerous synthetics have biological activity at dopamine, serotonin, and norepinephrine transporters. Importantly, monoamine transporters co-transport sodium ions along with their substrate, and movement of substrates and ions through the transporter can generate measurable ionic currents. Here we review how electrophysiological information has enabled us to determine how synthetic cathinones affect transporter-mediated currents in cells that express these transporters. Specifically, drugs that act as transporter substrates induce inward depolarizing currents when cells are held near their resting membrane potential, whereas drugs that act as transporter blockers induce apparent outward currents by blocking an inherent inward leak current. We have employed the two-electrode voltage-clamp technique in Xenopus laevis oocytes overexpressing monoamine transporters to determine whether synthetic cathinones found in the so-called bath salts products behave as blockers or substrates. We also examined the structure-activity relationships for synthetic cathinone analogs related to the widely abused compound MDPV, a common constituent in "bath salts" possessing potent actions at the dopamine transporter.

Authors+Show Affiliations

In Vivo Electrophysiology Unit, Behavioral Neuroscience Research Branch, National Institute on Drug Abuse - Intramural Research Program, National Institutes of Health, Triad Technology Center, 333 Cassell Drive, Suite 2200, Baltimore, MD, 21224, USA. ernesto.solisjr@nih.gov.

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural

Language

eng

PubMed ID

27677783

Citation

Solis, Ernesto. "Electrophysiological Actions of Synthetic Cathinones On Monoamine Transporters." Current Topics in Behavioral Neurosciences, vol. 32, 2017, pp. 73-92.
Solis E. Electrophysiological Actions of Synthetic Cathinones on Monoamine Transporters. Curr Top Behav Neurosci. 2017;32:73-92.
Solis, E. (2017). Electrophysiological Actions of Synthetic Cathinones on Monoamine Transporters. Current Topics in Behavioral Neurosciences, 32, 73-92. https://doi.org/10.1007/7854_2016_39
Solis E. Electrophysiological Actions of Synthetic Cathinones On Monoamine Transporters. Curr Top Behav Neurosci. 2017;32:73-92. PubMed PMID: 27677783.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Electrophysiological Actions of Synthetic Cathinones on Monoamine Transporters. A1 - Solis,Ernesto,Jr PY - 2016/9/30/pubmed PY - 2017/7/14/medline PY - 2016/9/29/entrez KW - Bath salts KW - Dopamine transporter KW - Serotonin transporter KW - Two-electrode voltage-clamp SP - 73 EP - 92 JF - Current topics in behavioral neurosciences JO - Curr Top Behav Neurosci VL - 32 N2 - Products containing psychoactive synthetic cathinones, such as mephedrone and 3,4-methylenedioxypyrovalerone (MDPV) are prevalent in our society. Synthetic cathinones are structurally similar to methamphetamine, and numerous synthetics have biological activity at dopamine, serotonin, and norepinephrine transporters. Importantly, monoamine transporters co-transport sodium ions along with their substrate, and movement of substrates and ions through the transporter can generate measurable ionic currents. Here we review how electrophysiological information has enabled us to determine how synthetic cathinones affect transporter-mediated currents in cells that express these transporters. Specifically, drugs that act as transporter substrates induce inward depolarizing currents when cells are held near their resting membrane potential, whereas drugs that act as transporter blockers induce apparent outward currents by blocking an inherent inward leak current. We have employed the two-electrode voltage-clamp technique in Xenopus laevis oocytes overexpressing monoamine transporters to determine whether synthetic cathinones found in the so-called bath salts products behave as blockers or substrates. We also examined the structure-activity relationships for synthetic cathinone analogs related to the widely abused compound MDPV, a common constituent in "bath salts" possessing potent actions at the dopamine transporter. SN - 1866-3370 UR - https://www.unboundmedicine.com/medline/citation/27677783/Electrophysiological_Actions_of_Synthetic_Cathinones_on_Monoamine_Transporters_ L2 - https://dx.doi.org/10.1007/7854_2016_39 DB - PRIME DP - Unbound Medicine ER -