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Defining the Propofol Binding Site Location on the GABAA Moez Bali and Myles H. Akabas
 

Summary: Defining the Propofol Binding Site Location on the GABAA
Receptor
Moez Bali and Myles H. Akabas
Departments of Physiology and Biophysics and of Neuroscience, Albert Einstein College of Medicine, Yeshiva University,
Bronx, New York
Received April 22, 2003; accepted October 7, 2003 This article is available online at http://molpharm.aspetjournals.org
ABSTRACT
The GABAA receptor is a target of many general anesthetics. The
low affinity of general anesthetics has complicated the search for
the location of anesthetic binding sites. Attention has focused on
two pairs of residues near the extracellular ends of the M2 and M3
membrane-spanning segments, 1Ser270/ 2Asn265 (15 M2)
and 1Ala291/ 2Met286 (M3). In the 4- resolution acetylcholine
receptor structure, the aligned positions are separated by 10 .
To determine whether these residues are part of a binding site for
propofol, an intravenous anesthetic, we probed propofol's ability
to protect cysteines substituted for these residues from modifica-
tion by the sulfhydryl-specific reagent p-chloromercuribenzene-
sulfonate (pCMBS ). pCMBS reacted with cysteines substituted
at the four positions in the absence and presence of GABA.

  

Source: Akabas, Myles - Department of Physiology and Biophysics, Albert Einstein College of Medicine, Yeshiva University

 

Collections: Biology and Medicine