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Neuropharmacology of Synthetic Cathinones.
Handb Exp Pharmacol. 2018; 252:113-142.HE

Abstract

Synthetic cathinones are derivatives of the naturally occurring compound cathinone, the main psychoactive ingredient in the khat plant Catha edulis. Cathinone is the β-keto analog of amphetamine, and all synthetic cathinones display a β-keto moiety in their structure. Several synthetic cathinones are widely prescribed medications (e.g., bupropion, Wellbutrin®), while others are problematic drugs of abuse (e.g., 4-methylmethcathinone, mephedrone). Similar to amphetamines, synthetic cathinones are psychomotor stimulants that exert their effects by impairing the normal function of plasma membrane transporters for dopamine (DAT), norepinephrine (NET), and 5-HT (SERT). Ring-substituted cathinones like mephedrone are transporter substrates that evoke neurotransmitter release by reversing the normal direction of transporter flux (i.e., releasers), whereas pyrrolidine-containing cathinones like 3,4-methylenedioxypyrovalerone (MDPV) are potent transporter inhibitors that block neurotransmitter uptake (i.e., blockers). Regardless of molecular mechanism, all synthetic cathinones increase extracellular monoamine concentrations in the brain, thereby enhancing cell-to-cell monoamine signaling. Here, we briefly review the mechanisms of action, structure-activity relationships, and in vivo pharmacology of synthetic cathinones. Overall, the findings show that certain synthetic cathinones are powerful drugs of abuse that could pose significant risk to users.

Authors+Show Affiliations

Designer Drug Research Unit (DDRU) NIDA, IRP, NIH, Baltimore, MD, USA. mbaumann@mail.nih.gov.Developmental, Cognitive and Behavioral Neuroscience, University of Houston, Houston, TX, USA.Center for Physiology and Pharmacology, Medical University of Vienna, Vienna, Austria.Center for Physiology and Pharmacology, Medical University of Vienna, Vienna, Austria.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30406443

Citation

Baumann, Michael H., et al. "Neuropharmacology of Synthetic Cathinones." Handbook of Experimental Pharmacology, vol. 252, 2018, pp. 113-142.
Baumann MH, Walters HM, Niello M, et al. Neuropharmacology of Synthetic Cathinones. Handb Exp Pharmacol. 2018;252:113-142.
Baumann, M. H., Walters, H. M., Niello, M., & Sitte, H. H. (2018). Neuropharmacology of Synthetic Cathinones. Handbook of Experimental Pharmacology, 252, 113-142. https://doi.org/10.1007/164_2018_178
Baumann MH, et al. Neuropharmacology of Synthetic Cathinones. Handb Exp Pharmacol. 2018;252:113-142. PubMed PMID: 30406443.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Neuropharmacology of Synthetic Cathinones. AU - Baumann,Michael H, AU - Walters,Hailey M, AU - Niello,Marco, AU - Sitte,Harald H, PY - 2018/11/9/pubmed PY - 2019/6/14/medline PY - 2018/11/9/entrez KW - Cathinone KW - Dopamine KW - Monoamine KW - Serotonin KW - Stimulant KW - Transporter SP - 113 EP - 142 JF - Handbook of experimental pharmacology JO - Handb Exp Pharmacol VL - 252 N2 - Synthetic cathinones are derivatives of the naturally occurring compound cathinone, the main psychoactive ingredient in the khat plant Catha edulis. Cathinone is the β-keto analog of amphetamine, and all synthetic cathinones display a β-keto moiety in their structure. Several synthetic cathinones are widely prescribed medications (e.g., bupropion, Wellbutrin®), while others are problematic drugs of abuse (e.g., 4-methylmethcathinone, mephedrone). Similar to amphetamines, synthetic cathinones are psychomotor stimulants that exert their effects by impairing the normal function of plasma membrane transporters for dopamine (DAT), norepinephrine (NET), and 5-HT (SERT). Ring-substituted cathinones like mephedrone are transporter substrates that evoke neurotransmitter release by reversing the normal direction of transporter flux (i.e., releasers), whereas pyrrolidine-containing cathinones like 3,4-methylenedioxypyrovalerone (MDPV) are potent transporter inhibitors that block neurotransmitter uptake (i.e., blockers). Regardless of molecular mechanism, all synthetic cathinones increase extracellular monoamine concentrations in the brain, thereby enhancing cell-to-cell monoamine signaling. Here, we briefly review the mechanisms of action, structure-activity relationships, and in vivo pharmacology of synthetic cathinones. Overall, the findings show that certain synthetic cathinones are powerful drugs of abuse that could pose significant risk to users. SN - 0171-2004 UR - https://www.unboundmedicine.com/medline/citation/30406443/Neuropharmacology_of_Synthetic_Cathinones_ L2 - https://dx.doi.org/10.1007/164_2018_178 DB - PRIME DP - Unbound Medicine ER -