Article
Mutation of the GABAA receptor M1 transmembrane proline increases GABA affinity and reduces barbiturate enhancement.
Neuropharmacology - 1 Mar 2002
Greenfield L John, Zaman Shahid H, Sutherland Margaret L, Lummis Sarah C R, Niemeyer María-Isabel, Barnard Eric A, Macdonald Robert L
Abstract excerpt
All GABA(A) receptor (GABAR) subunits include an invariant proline in a consensus motif in the first transmembrane segment (M1). In receptors containing bovine alpha1, beta1 and gamma2 subunits, we analyzed the effect of mutating this M1 proline to alanine in the alpha1 or beta1 subunit using 3 different expression systems. The beta1 subunit mutant, beta1(P228A), reduced the EC(50) for GABA about 10-fold in whole...
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