Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships for the side-chain.

Affiliation

Auckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, New Zealand. Electronic address: [Email]

Abstract

N-Aliphatic ester analogues of the non-opioid ketamine (1) retain effective anaesthetic/analgesic properties while minimising ketamine's psychomimetic side-effects. We show that the anaesthetic/analgesic properties of these ester analogues depend critically on the length (from 2 to 4 carbons), polarity and steric cross-section of the aliphatic linker chain. More stable amide and ethylsulfone analogues generally showed weaker anaesthetic/analgesic activity. There was no correlation between the anaesthetic/analgesic properties of the compounds and their binding affinities for the N-methyl-d-aspartate (NMDA) receptor.

Keywords

Anaesthesia,Esters,Ketamine,Short-acting,Structure-activity relationship,

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