Muscimol (also known as Agarin) is a potent and selective GABA(A) receptor agonist and a partial agonist of GABA(C) receptor^1,2. 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 drugs^1,3.