BQCA

Highly selective allosteric potentiator of the M₁ muscarinic acetylcholine receptor (mAChR). Reduces the concentration of ACh required to activate M₁ up to 129-fold and displays no potentiation, agonism or antagonism activity at other mAChRs at concentrations up to 100µM. Reverses scopolamine-induced memory deficits and increases blood flow to the cerebral cortex in mouse models. M₁ activators slow the progression of Alzheimers disease. Induces β-arrestin recruitment to M₁. At 100µM, it activated M₁ in the absence of ACh to ca. 50% maximal response. At 10µM, it reduced the concentration of ACh required to displace radioligand by 45-fold. In vivo experiments were carried out in mice at 15 or 20mg/kg. The compound is cell permeable, brain penetrant and orally active.