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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. 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. Etomidate did not affect either type of receptor at clinically relevant concentrations, whereas carboetomidate concentrations near 50% effective concentration for anesthesia significantly inhibited nnAChRs. Compared with etomidate, carboetomidate's higher hydrophobicity is associated with greater inhibition of nnAChRs.
Belelli,
The in vitro and in vivo enantioselectivity of etomidate implicates the GABAA receptor in general anaesthesia.
2003, Pubmed,
Xenbase
Belelli,
The in vitro and in vivo enantioselectivity of etomidate implicates the GABAA receptor in general anaesthesia.
2003,
Pubmed
,
Xenbase
Cotten,
Carboetomidate: a pyrrole analog of etomidate designed not to suppress adrenocortical function.
2010,
Pubmed
,
Xenbase
Dutton,
Do N-methyl-D-aspartate receptors mediate the capacity of inhaled anesthetics to suppress the temporal summation that contributes to minimum alveolar concentration?
2006,
Pubmed
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2002,
Pubmed
Flood,
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Pubmed
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Xenbase
Hill-Venning,
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1997,
Pubmed
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Xenbase
Jurd,
General anesthetic actions in vivo strongly attenuated by a point mutation in the GABA(A) receptor beta3 subunit.
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Pubmed
O'Connell,
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2011,
Pubmed
,
Xenbase
Pejo,
In vivo and in vitro pharmacological studies of methoxycarbonyl-carboetomidate.
2012,
Pubmed
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Xenbase
Raines,
Nonhalogenated anesthetic alkanes and perhalogenated nonimmobilizing alkanes inhibit alpha(4)beta(2) neuronal nicotinic acetylcholine receptors.
2002,
Pubmed
,
Xenbase
Solt,
Differential modulation of human N-methyl-D-aspartate receptors by structurally diverse general anesthetics.
2006,
Pubmed
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Xenbase
Zhang,
Blockade of acetylcholine receptors does not change the dose of etomidate required to produce immobility in rats.
2007,
Pubmed
