Carboetomidate inhibits alpha4/beta2 neuronal nicotinic acetylcholine receptors at concentrations affecting animals
Language: 
English
Abstract: 

BACKGROUND: Carboetomidate is an etomidate derivative that produces hypnosis without inhibiting adrenal corticosteroid synthesis. Similar to etomidate, carboetomidate modulates ?-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.

Author(s): 
Pierce, David W.
Pejo, Ervin
Raines, Douglas E.
Forman, Stuart A.
Item Type: 
Journal Article
Publication Title: 
Anesthesia and Analgesia
Journal Abbreviation: 
Anesth. Analg.
Publication Date: 
7/12/2015
Publication Year: 
2012
Pages: 
70-72
Volume: 
115
Issue: 
1
ISSN: 
1526-7598
DOI: 
10.1213/ANE.0b013e318254273e
Library Catalog: 
PubMed
Extra: 
PMID: 22543065 PMCID: PMC3381859

Turabian/Chicago Citation

David W. Pierce, Ervin Pejo, Douglas E. Raines and Stuart A. Forman. 7/12/2015. "Carboetomidate inhibits alpha4/beta2 neuronal nicotinic acetylcholine receptors at concentrations affecting animals." Anesthesia and Analgesia 115: 1: 70-72. 10.1213/ANE.0b013e318254273e.

Wikipedia Citation

<ref> {{Cite journal | doi = 10.1213/ANE.0b013e318254273e | issn = 1526-7598 | volume = 115 | pages = 70-72 | last = Pierce | first = David W. | coauthors = Pejo, Ervin, Raines, Douglas E., Forman, Stuart A. | title = Carboetomidate inhibits alpha4/beta2 neuronal nicotinic acetylcholine receptors at concentrations affecting animals | journal = Anesthesia and Analgesia | date = 7/12/2015 | pmid = | pmc = }} </ref>