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 |
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Formula: | C18H15NO4 |
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MW: | 309.3 |
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Source: | Synthetic. |
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CAS: | 338747-41-4 |
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Purity: | ≥97% (HPLC) |
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Appearance: | White solid. |
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Solubility: | Soluble in DMSO (10mg/ml). |
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Shipping: | Ambient Temperature |
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Long Term Storage: | Ambient |
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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. |
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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;