BQCA

BQCA is a highly selective positive allosteric modulator of the M₁ muscarinic acetylcholine receptor (mAChR), as it dose-dependently reduces the concentration of acetylcholine required to activate the M₁ receptor.¹ The effective range for potentiation of M₁ in cells by BQCA is 0.1 to 100 μM with an inflection point value of 845 nM when 3 nM acetylcholine is used.¹ BQCA displays no potentiation, agonism, or antagonism at other mAChRs at concentrations up to 100 μM.¹ It has excellent brain penetration and increases the firing rate of medial prefrontal cortex neurons in vivo in rats.² BQCA prevents scopolamine-induced memory deficits in both contextual fear conditioning and a spontaneous alternation task in mice.^1,3 It also restores impairment in reversal learning in a mouse model of Alzheimer’s disease and improves memory performance in rats.^2,4

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1. Ma, L., Seager, M.A., Wittman, M., et al. Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proc. Natl. Acad. Sci. USA 106(37), 15950-15955 (2009).

2. Shirey, J.K., Brady, A.E., Jones, P.J., et al. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning. J. Neurosci. 29(45), 14271-14286 (2009).

3. Chambon, C., Jatzke, C., Wegener, N., et al. Using cholinergic M1 receptor positive allosteric modulators to improve memory via enhancement of brain cholinergic communication. Eur. J. Pharmacol. 697(1-3), 73-80 (2012).

4. Galloway, C.R., Lebois, E.P., Shagarabi, S., et al. Effects of selective activation of M1 and M₄ muscarinic receptors on object recognition memory performance in rats. Pharmacology 93(1-2), 57-64 (2014).