GMQ (hydrochloride)

GMQ is an activator of acid-sensing ion channel 3 (ASIC3).¹ It evokes rapid inward currents with little desensitization in CHO cells expressing ASIC3 (EC₅₀ = 67 µM at neutral pH). It is also an inhibitor of the GABA_A receptor (IC₅₀ = 0.39 µM in primary rat hippocampal neurons).² GMQ has stimulatory effects on large-conductance calcium-activated potassium (K_Ca1.1/BK_Ca) channels in GH3 rat pituitary cells and on non-selective cation currents in Rolf B1.T olfactory sensory neurons.³ It increases paw licking time in Asic3^+/+ and, to a lesser extent, Asic3^-/- mice when administered at a dose of 100 µM, an effect that can be blocked by the ASIC inhibitor amiloride (Item No. 14409).¹

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1. Yu, Y., Chen, Z., Li, W.G., et al. A nonproton ligand sensor in the acid-sensing ion channel. Neuron 68(1), 61-72 (2010).

2. Xiao, X., Zhu, M.X., and Xu, T.L. 2-Guanidine-4-methylquinazoline acts as a novel competitive antagonist of A type γ-aminobutyric acid receptors. Neuropharmacology 75, 126-137 (2013).

3. So, E.C., Wang, Y., Yang, L.Q., et al. Multiple regulatory actions of 2-guanidine-4-methylquinazoline (GMQ), an agonist of acid-sensing ion channel type 3, on ionic currents in pituitary GH3 cells and in olfactory sensory (Rolf B₁.T) neurons. Biochem. Pharmacol. 151, 79-88 (2018).