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.
    Structure
    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.
    References
    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