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- W2041353739 abstract "ELIC is a prokaryotic pentameric ligand gated ion channel (pLGIC) homologous to Cys-loop receptors, which are molecular targets of general anesthetics and alcohols. Crystal structures of ELIC and its complex with the antagonist acetylcholine have been resolved recently, suggesting the possibility of using ELIC to understand the structural basis of anesthetic and alcohol modulation on pLGICs. However, the pharmacological profiles of ELIC for modulation by general anesthetics and alcohols have not been well defined. In this study, we characterized these profiles for ELIC expressed in Xenopus laevis oocytes with two-electrode voltage clamp techniques. We found that the ELIC current elicited by the agonist propylamine could be inhibited by both volatile and intravenous general anesthetics at clinically relevant concentrations. ELIC is also inhibited by ethanol and other n-alcohols with potency increasing with the number of carbons until n-nonanol, where inhibition is cut off. Alcohol modulation on ELIC is similar to that on GABAR-ρ1 but different from nAChRs, which are potentiated by ethanol. In addition, ELIC is inhibited by the benzodiazepine drug diazepam. In summary, ELIC shares some pharmacological characteristics of cation-conducting eukaryotic pLGICs and is a suitable model for the structural study of the actions of general anesthetics and alcohols on pLGICs. Supported by NIH (R01GM066358, R01GM056257, and R37GM049202)." @default.
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- W2041353739 date "2013-01-01" @default.
- W2041353739 modified "2023-09-29" @default.
- W2041353739 title "Functional Modulation of the ELIC by General Anesthetics and Alcohols" @default.
- W2041353739 doi "https://doi.org/10.1016/j.bpj.2012.11.3511" @default.
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