The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor

Roth, Bryan L., Gibbons, Simon, Arunotayanun, Warunya, Huang, Xi Ping, Setola, Vincent, Treble, Ric and Iversen, Les (2013) The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor. PLoS One, 8 (3). ISSN 1932-6203

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Abstract

In this paper we determined the pharmacological profiles of novel ketamine and phencyclidine analogues currently used as 'designer drugs' and compared them to the parent substances via the resources of the National Institute of Mental Health Psychoactive Drug Screening Program. The ketamine analogues methoxetamine ((RS)-2-(ethylamino)-2-(3-methoxyphenyl)cyclohexanone) and 3-MeO-PCE (N-ethyl-1-(3-methoxyphenyl)cyclohexanamine) and the 3- and 4-methoxy analogues of phencyclidine, (1-[1-(3-methoxyphenyl)cyclohexyl]piperidine and 1-[1-(4-methoxyphenyl)cyclohexyl]piperidine), were all high affinity ligands for the PCP-site on the glutamate NMDA receptor. In addition methoxetamine and PCP and its analogues displayed appreciable affinities for the serotonin transporter, whilst the PCP analogues exhibited high affinities for sigma receptors. Antagonism of the NMDA receptor is thought to be the key pharmacological feature underlying the actions of dissociative anaesthetics. The novel ketamine and PCP analogues had significant affinities for the NMDA receptor in radioligand binding assays, which may explain their psychotomimetic effects in human users. Additional actions on other targets could be important for delineating side-effects.

Item Type: Article
Additional Information: Correction: 22 Mar 2018: Roth BL, Gibbons S, Arunotayanun W, Huang XP, Setola V, et al. (2018) Correction: The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor. PLOS ONE 13(3): e0194984. https://doi.org/10.1371/journal.pone.0194984
Uncontrolled Keywords: biochemistry, genetics and molecular biology(all),agricultural and biological sciences(all),general ,/dk/atira/pure/subjectarea/asjc/1300
Faculty \ School: Faculty of Science > School of Pharmacy
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Depositing User: LivePure Connector
Date Deposited: 14 Jul 2020 23:51
Last Modified: 14 Jul 2020 23:51
URI: https://ueaeprints.uea.ac.uk/id/eprint/76059
DOI: 10.1371/journal.pone.0059334

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