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Arylcyclohexylamine Derivatives: Pharmacokinetic, Pharmacodynamic, Clinical and Forensic Aspects

Romain Pelletier, Brendan Le Daré, Diane Le Bouëdec, Angéline Kernalléguen, Pierre‐Jean Ferron, Isabelle Morel, Thomas Gicquel

2022International Journal of Molecular Sciences26 citationsDOIOpen Access PDF

Abstract

Since the 2000s, an increasing number of new psychoactive substances (NPS) have appeared on the drug market. Arylcyclohexylamine (ACH) compounds such as ketamine, phencyclidine and eticyclidine derivatives are of particular concern, given their rapidly increasing use and the absence of detailed toxicity data. First used mainly for their pharmacological properties in anesthesia, their recreational use is increasing. ACH derivatives have an antagonistic activity against the N-methyl-D-aspartate receptor, which leads to dissociative effects (dissociation of body and mind). Synthetic ketamine derivatives produced in Asia are now arriving in Europe, where most are not listed as narcotics and are, thus, legal. These structural derivatives have pharmacokinetic and pharmacodynamic properties that are sometimes very different from ketamine. Here, we describe the pharmacology, epidemiology, chemistry and metabolism of ACH derivatives, and we review the case reports on intoxication.

Topics & Concepts

PhencyclidineDissociativeKetaminePharmacologyPharmacodynamicsPharmacokineticsDrugChemistryMedicineNMDA receptorReceptorAnesthesiaBiochemistryTreatment of Major DepressionPsychedelics and Drug StudiesPharmacological Receptor Mechanisms and Effects
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