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.
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.
Authors: Robert C Dutton; Michael J Laster; Yilei Xing; James M Sonner; Douglas E Raines; Ken Solt; Edmond I Eger Journal: Anesth Analg Date: 2006-05 Impact factor: 5.108
Authors: Ervin Pejo; Joseph F Cotten; Elizabeth W Kelly; Ri Le Ge; Gregory D Cuny; Joydev K Laha; Jifeng Liu; Xiang Jie Lin; Douglas E Raines Journal: Anesth Analg Date: 2011-09-29 Impact factor: 5.108
Authors: Xiaoxuan Yang; Youssef Jounaidi; Jennifer B Dai; Francisco Marte-Oquendo; Elizabeth S Halpin; Lauren E Brown; Richard Trilles; Wenqing Xu; Renee Daigle; Buwei Yu; Scott E Schaus; John A Porco; Stuart A Forman Journal: Anesthesiology Date: 2018-09 Impact factor: 7.892