Overview
- Middendorp, S.J. et al. (2015) Neuropharmacology 95, 459.
Alomone Labs SJM-3 potentiates 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). Currents are significantly enhanced by co-application of 50 µM SJM-3 (#S-215), as indicated (bar), at a holding potential of -60 mV.
- Middendorp, S.J. et al. (2015) Neuropharmacology 95, 459.
- Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry 56, 35.
SJM-3 is a positive allosteric modulator of γ-aminobutyric acid type A (GABA(A)) receptors. It potentiates GABA(A) receptor currents by binding at the diazepam binding site in the transmembrane domain. SJM-3 was also shown to act as an antagonist at the α+/γ− site of the receptor1.
GABA(A) receptors belong to the cys-loop pentameric ligand-gated ion channel family. These receptors are major inhibitory neurotransmitter receptors in the brain and in the mammalian central nervous system and are responsible for mediating GABA action. They are composed of five homologous subunits that are arranged around a central chloride-selective pore. GABA(A) receptors are important targets for many clinical drugs1,2.
SJM-3 (#S-215) is a highly pure, synthetic, and biologically active compound.
Powered by Bioz
