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Acetylcholine receptor activator
BML-C121-0010 10 mg 134.00 USD
BML-C121-0050 50 mg 537.00 USD
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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.

Product Details

Alternative Name:1-(4-Methoxybenzyl)-4-oxo-1,4-dihydro-3-quinoline carboxylic acid, Benzyl quinolone carboxylic acid
Purity:≥97% (HPLC)
Appearance:White solid.
Solubility:Soluble in DMSO (10mg/ml).
Shipping:Ambient Temperature
Long Term Storage:Ambient
Use/Stability:Stable for at least 1 year after receipt when stored at room temperature. Stock solutions are stable for for up to 3 months at -20°C.
Regulatory Status:RUO - Research Use Only
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Product Literature References

Activation of basal forebrain cholinergic neurons improves colonic hyperpermeability through the vagus nerve and adenosine A2B receptors in rats: M. Ishioh, et al.; Biochem. Pharmacol. 206, 115331 (2022), Abstract;
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.: L. Ma, et al.; PNAS 106, 15950 (2009), Abstract; Full Text
Cholinergic treatments with emphasis on m1 muscarinic agonists as potential disease-modifying agents for Alzheimer's disease.: A. Fisher; Neurotherapeutics 5, 433 (2008), Abstract;

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