U 93631

An Antagonist of GABA(A) and 5-HT3A Receptors
  • New
Cat #: U-120
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 299.37 Da.
    Purity >99%.
    Effective concentration 1-10 µM.
    Chemical name tert-butyl 4,4-dimethyl-5H-imidazo[1,5-a]quinoxaline-3-carboxylate.
    Molecular formula C17H21N3O2.
    CAS number 152273-12-6.
    Activity U 93631 is a ligand at the picrotoxin site of GABA(A) receptors, allosterically antagonizing GABA-induced Cl- currents by decreasing single-channel open probability1 and accelerating current decay (Kd = 2 µM)2. It is also an antagonist of 5-HT3A receptors (IC50 = 50 µM)3.
    Storage before reconstitution Product before reconstitution should be stored at -20°C.
    Reconstitution Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).
    Storage after reconstitution Up to three months at -20°C.
    Our bioassay
    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.
    1. Dillon, G.H. et al. (1995) J. Pharmacol. Exp. Ther. 272, 597.
    2. Dillon, G.H. et al. (1993) Mol. Pharmacol. 44, 860.
    3. Williams, M. et al. (1989) J. Pharmacol. Exp. Ther. 248, 89.
    4. Das, P. et al. (2003) Neuropharmacology 44, 431.
    Target: GABA(A), 5-HT3A receptors
    Last update: 08/02/2018

    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.

    Alomone Labs is pleased to offer U 93631 (#U-120).

    For research purposes only, not for human use