Overview
- Mortensen, M. et al. (2010) J. Physiol. 588, 1251.
- Wang, J. et al. (2007) J. Biol. Chem. 282, 26210.
Alomone Labs Muscimol hydrobromide activates GABA(A) receptors expressed in Xenopus oocytes.Time course of GABA(A) α1/β2 currents, reversibly activated in a concentration dependent manner by 0.01 µM, 0.1 µM and 1 µM Muscimol hydrobromide (#M-240) while membrane potential was held at -60 mV.
Muscimol (also known as Agarin) is a potent and selective GABA(A) receptor agonist and a partial agonist of GABA(C) receptor1,2. It activates the receptors through a structural transition from the closed to the open state. Muscimol demonstrates potency with EC50 values of 0.92 µM on α1/β3/γ2 receptor and 0.20 µM on α4/β/3δ receptor2.
The compound is extracted from the mushroom Amanita muscaria as a psychotropic drug and is being used as a local anesthetic drug. Studies have shown the effectiveness of muscimol for reduction of neuropathic pain symptoms1.
GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate the actions of GABA, a major inhibitory neurotransmitter, in the central nervous system. The GABA(A) receptor is considered to be a major target of antiseizure drugs1,3.
