Photo-activated azi-etomidate, a general anesthetic photolabel, irreversibly enhances gating and desensitization of gamma-aminobutyric acid type A receptors.

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Abstract

The general anesthetic etomidate acts via gamma-aminobutyric acid type A (GABA(A)) receptors, enhancing activation at low GABA and prolonging deactivation. Azi-etomidate is a photo-reactive etomidate derivative with similar pharmacological actions, which has been used to identify putative binding sites. The authors examine the irreversible effects of azi-etomidate photo-modification on functional GABA(A) receptors in cell membranes.

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Journal

Journal ID (iso-abbrev): Anesthesiology

Title: Anesthesiology

Publisher: Ovid Technologies (Wolters Kluwer Health)

ISSN (Electronic): 1528-1175

ISSN (Print): 0003-3022

Publication date (Electronic): Jan 2008

Volume: 108

Issue: 1

Affiliations

[1 ] Department of Anesthesia & Critical Care, Massachusetts General Hospital, Boston, Massachusetts 02114, USA.

Article

Publisher Item ID: 00000542-200801000-00017 Mid ID: NIHMS70343

DOI: 10.1097/01.anes.0000296074.33999.52

PMC ID: 2564603

PubMed ID: 18156888

SO-VID: 87908bd0-3e0a-48e2-bd18-2aba207bf836

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