Overview
- Dillon, G.H. et al. (1995) J. Pharmacol. Exp. Ther. 272, 597.
- Dillon, G.H. et al. (1993) Mol. Pharmacol. 44, 860.
- Das, P. et al. (2003) Neuropharmacology 44, 431.
Alomone Labs U 93631 inhibits GABA(A) receptors expressed in Xenopus oocytes.Representative time course of GABA(A) α1/β2 current, activated by a continuous application (top dotted line) of 0.1 µM γ-aminobutyric acid (#G-110), and reversibly inhibited by 2 µM and 10 µM U 93631 (#U-120), as indicated (bar), at a holding potential of -60 mV.
U 93631 is a synthetic compound that acts as an antagonist of the gamma-aminobutyric acid type A GABA(A) receptors and of 5-hydroxytryptamine type 3A (5-HT3A) receptors, displaying an IC50 of 50 µM for the serotonin receptor4. The compound accelerates the decay of GABA induced currents through an allosteric manner. The properties of U 93631 are shown to be analogous to those of picrotoxin and both share overlapping binding domains1,2.
GABA(A) receptors and 5-HT3 (serotonin-gated) receptor channels are members of the Cys-loop superfamily of ligand-gated ion channels. These receptors are expressed throughout the central and peripheral nervous systems and mediate a variety of important physiological functions. GABA(A) receptors mediate the actions of GABA, a major inhibitory neurotransmitter. 5-HT3 receptors mediate those of serotonin3.
