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Papers of the Week


2019 Dec 19


BMC Pharmacol Toxicol


20


1

KEA-1010, a ketamine ester analogue, retains analgesic and sedative potency but is devoid of Psychomimetic effects.

Authors

Harvey M, Sleigh J, Voss L, Bickerdike M, Dimitrov I, Denny W
BMC Pharmacol Toxicol. 2019 Dec 19; 20(1):85.
PMID: 31856925.

Abstract

Ketamine, a widely used anaesthetic and analgesic agent, is known to improve the analgesic efficacy of opioids and to attenuate central sensitisation and opioid-induced hyperalgesia. Clinical use is, however, curtailed by unwanted psychomimetic effects thought to be mediated by N-methyl-D-aspartate (NMDA) receptor antagonism. KEA-1010, a ketamine ester-analogue designed for rapid offset of hypnosis through hydrolysis mediated break-down, has been shown to result in short duration sedation yet prolonged attenuation of nociceptive responses in animal models. Here we report on behavioural effects following KEA-1010 administration to rodents.