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Updated: May 22, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
Published on: February 11, 2019
Carboetomidate inhibits alpha4/beta2 neuronal nicotinic acetylcholine receptors at concentrations affecting animals
David W Pierce1, Ervin Pejo, Douglas E Raines
1Department of Anesthesia, Critical Care and Pain Medicine, Jackson 444, Massachusetts General Hospital, 55 Fruit St., Boston, MA 02114, USA.
Background:
Carboetomidate 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.
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.
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