Article
Mutational Analysis of the Putative High-Affinity Propofol Binding Site in Human β3 Homomeric GABAA Receptors.
Molecular pharmacology - 1 Oct 2015
Eaton Megan M, Cao Lily Q, Chen Ziwei, Franks Nicholas P, Evers Alex S, Akk Gustav
Abstract excerpt
Propofol is a sedative and anesthetic agent that can both activate GABA(A) receptors and potentiate receptor activation elicited by submaximal concentrations of the transmitter. A recent modeling study of the β3 homomeric GABA(A) receptor postulated a high-affinity propofol binding site in a hydrophobic pocket in the middle of a triangular cleft lined by the M1 and M2 membrane-spanning domains of one subunit and...
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