ASIC Channel Modulator II, GMQ

Primary Target
ASIC3

Reversible: yes

Toxicity: Standard Handling (A)

A positively charged guanidium-containing quinazoline that modulates ASIC function by blocking acid-induced maximal peak current as well as by altering ASICs pH dependence for activation and inactivation, enabling a partial, but sustained ASIC3 activation around neutral pH (4.4% of pH 5-induced peak current with 1 mM GMQ at pH 7.4), which is inhibitable by Amiloride (Cat. No. 129876). Intraplantar paw injection (10 µL 100 µM) is reported to elicit a pain response in asic3^+/+, but not asic3^-/-, mice in vivo. GMQ targeting area appears to overlap with Amiloride binding site in the pore region, but is distinct from ASIC calcium binding site.

Alijevic, O., and Kellenberger, S. 2012. J Biol Chem.287, 36059.

Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol.303, C699.
Yu, Y., et al. 2010. Neuron.68, 61.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

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