U 93631

An Antagonist of GABA(A) and 5-HT3A Receptors
Cat #: U-120
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
Source: Synthetic
MW: 299.37 Da.
Target: GABA(A), 5-HT3A receptors
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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 domains^1,2.

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).

U 93631References

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) Neuropharmacology44, 431.

• Our Bioassay
• Specifications
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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.
Purity>99%.
Effective concentration1-10 µM.
Chemical nametert-butyl 4,4-dimethyl-5H-imidazo[1,5-a]quinoxaline-3-carboxylate.
Molecular formulaC₁₇H₂₁N₃O₂.
CAS number152273-12-6.
ActivityU 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 (K_d = 2 µM)². It is also an antagonist of 5-HT3A receptors (IC₅₀ = 50 µM)³.
Storage before reconstitutionProduct before reconstitution should be stored at -20°C.
ReconstitutionSoluble in DMSO. Centrifuge before use (10000 x g, 5 min).
Storage after reconstitutionUp to three months at -20°C.