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PQCA 

Cat. No. M27841
PQCA  Structure
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Biological Activity

PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.

Chemical Information
Molecular Weight 388.42
Formula C22H20N4O3
CAS Number 1144504-35-7
Form Solid
Solubility (25°C) DMSO 10 mg/mL (ultrasonic and warming and heat to 60°C)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Anastasios Peppas, et al. Dalton Trans. Sterically demanding pyridine-quinoline anchoring ligands as building blocks for copper(I)-based dye-sensitized solar cell (DSSC) complexes

[2] Henry S Lange, et al. J Pharmacol Exp Ther. The M1 Muscarinic Positive Allosteric Modulator PQCA Improves Performance on Translatable Tests of Memory and Attention in Rhesus Monkeys

[3] Vanita Puri, et al. Behav Brain Res. The selective positive allosteric M1 muscarinic receptor modulator PQCA attenuates learning and memory deficits in the Tg2576 Alzheimer's disease mouse model

[4] Joshua D Vardigan, et al. Psychopharmacology (Berl). Improved cognition without adverse effects: novel M1 muscarinic potentiator compares favorably to donepezil and xanomeline in rhesus monkey

[5] Jason M Uslaner, et al. Psychopharmacology (Berl). The muscarinic M1 receptor positive allosteric modulator PQCA improves cognitive measures in rat, cynomolgus macaque, and rhesus macaque

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