酮酯和酰胺类作为短效麻醉剂：侧链的结构-活性关系。
Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships for the side-chain.
机构信息
Auckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, New Zealand.
Waikato Clinical School, University of Auckland, New Zealand.
出版信息
Bioorg Med Chem. 2019 Apr 1;27(7):1226-1231. doi: 10.1016/j.bmc.2019.02.010. Epub 2019 Feb 5.
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.
N-脂族酯类似物的非阿片类氯胺酮 (1) 保留有效的麻醉/镇痛特性，同时最大限度地减少氯胺酮的致幻副作用。我们表明，这些酯类似物的麻醉/镇痛特性取决于脂肪族连接链的长度（从 2 到 4 个碳原子）、极性和空间位阻。更稳定的酰胺和乙基砜类似物通常表现出较弱的麻醉/镇痛活性。化合物的麻醉/镇痛性质与其对 N-甲基-D-天冬氨酸 (NMDA) 受体的结合亲和力之间没有相关性。
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