Carboetomidate Inhibits Alpha4/Beta2 Neuronal Nicotinic Acetylcholine Receptors at Concentrations Affecting Animals

被引：7

作者：

Pierce, David W. ^{[1
]}

Pejo, Ervin ^{[1
]}

Raines, Douglas E. ^{[1
]}

Forman, Stuart A. ^{[1
]}

机构：

[1] Massachusetts Gen Hosp, Dept Anesthesia Crit Care & Pain Med, Boston, MA 02114 USA

来源：

ANESTHESIA AND ANALGESIA | 2012年 / 115卷 / 01期

关键词：

D-ASPARTATE RECEPTORS; INHALED ANESTHETICS; ETOMIDATE; SUPPRESS; MEDIATE;

D O I：

10.1213/ANE.0b013e318254273e

中图分类号：

R614 [麻醉学];

学科分类号：

100217 [麻醉学];

摘要：

BACKGROUND: Carboetomidate is an etomidate derivative that produces hypnosis without inhibiting adrenal corticosteroid synthesis. Similar to etomidate, carboetomidate modulates gamma-aminobutyric acid type A receptors, but its effects on other ion channel targets of general anesthetics are unknown. METHODS: We compared etomidate and carboetomidate effects on human N-methyl-D-aspartate receptors or neuronal nicotinic acetylcholine receptors (nnAChRs) expressed in Xenopus oocytes, using 2-microelectrode voltage clamp electrophysiology. RESULTS: Etomidate did not affect either type of receptor at clinically relevant concentrations, whereas carboetomidate concentrations near 50% effective concentration for anesthesia significantly inhibited nnAChRs. CONCLUSIONS: Compared with etomidate, carboetomidate's higher hydrophobicity is associated with greater inhibition of nnAChRs. (Anesth Analg 2012;115:70-2)

引用

页码：70 / 72

页数：3

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