A single phenylalanine residue in the main intracellular loop of α1 γ-aminobutyric acid type A and glycine receptors influences their sensitivity to propofol

G Moraga-Cid, GE Yevenes, G Schmalzing… - The Journal of the …, 2011 - pubs.asahq.org
Background The intravenous anesthetic propofol acts as a positive allosteric modulator of
glycine (GlyRs) and γ-aminobutyric acid type A (GABAARs) receptors. Although the role of
transmembrane residues is recognized, little is known about the involvement of other
regions in the modulatory effects of propofol. Therefore, the influence of the large
intracellular loop in propofol sensitivity of both receptors was explored. Methods The large
intracellular loop of α1 GlyRs and α1β2 GABAARs was screened using alanine …