ASIC Channel Modulator II, GMQ

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.

Primary Target
ASIC3

Reversible: yes

Toxicity: Standard Handling (A)

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

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.

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