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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
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Xenbase
Cotten,
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Pubmed
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Xenbase
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Pubmed
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Xenbase
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Xenbase
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Pubmed
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Xenbase
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Pubmed
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Xenbase
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Pubmed
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Xenbase
Solt,
Differential modulation of human N-methyl-D-aspartate receptors by structurally diverse general anesthetics.
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Pubmed
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Xenbase
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Pubmed
