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Anesthesia and analgesia · Jul 2012
Comparative StudyCarboetomidate inhibits alpha4/beta2 neuronal nicotinic acetylcholine receptors at concentrations affecting animals.
- David W Pierce, Ervin Pejo, Douglas E Raines, and Stuart A Forman.
- Department of Anesthesia, Critical Care and Pain Medicine, Jackson 444, Massachusetts General Hospital, 55 Fruit St., Boston, MA 02114, USA.
- Anesth. Analg.. 2012 Jul 1;115(1):70-2.
BackgroundCarboetomidate is an etomidate derivative that produces hypnosis without inhibiting adrenal corticosteroid synthesis. Similar to etomidate, carboetomidate modulates γ-aminobutyric acid type A receptors, but its effects on other ion channel targets of general anesthetics are unknown.MethodsWe 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.ResultsEtomidate did not affect either type of receptor at clinically relevant concentrations, whereas carboetomidate concentrations near 50% effective concentration for anesthesia significantly inhibited nnAChRs.ConclusionsCompared with etomidate, carboetomidate's higher hydrophobicity is associated with greater inhibition of nnAChRs.
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