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PQCA

Names

[ CAS No. ]:
1144504-35-7

[ Name ]:
PQCA

[Synonym ]:
1-((4-cyano-4-(pyridin-2-yl)piperidin-1-yl)methyl)-4-oxo-4H-quinolizine-3-carboxylic acid
1-[(4-cyano-4-(pyridin-2-yl)piperidin-1-yl)methyl]-4-oxo-4H-quinolizine-3-carboxylate
1-(4-cyano-4-(pyridine-2-yl)piperidin-1-yl)methyl-4-oxo-4 H-quinolizine-3-carboxylic acid
1-[(4-cyano-4-pyridin-2-ylpiperidin-1-yl)methyl]-4-oxo-4H-quinolizine-3-carboxylic acid

Biological Activity

[Description]:

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, and is inactive for other muscarinic receptors. PQCA improves cognitive performance and cerebral blood flow in rat, cynomolgus macaque, and rhesus macaque. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR
Signaling Pathways >> GPCR/G Protein >> mAChR
Research Areas >> Neurological Disease

[Target]

EC50: 49 nM (Rhesus M1 receptor) and 135 nM (Human M1 receptor)[1]


[In Vivo]

PQCA (3-30 mg/kg; Oral administration; single- or pair-housed male rhesus monkeys) treatment attenuates the scopolamine deficits in PAL and CPT tasks. Blockade of muscarinic signaling by scopolamine produces significant impairments in both tasks[1]. Animal Model: Ten single- or pair-housed male rhesus monkeys (6-10 years old; 5.2-10.5 kg) with scopolamine[1] Dosage: 3 mg/kg, 10 mg/kg, or 30 mg/kg Administration: Oral administration Result: Attenuated the scopolamine deficits in paired-associates learning (PAL) and the continuous-performance task (CPT).

[References]

[1]. Lange HS, et al. The M1 Muscarinic Positive Allosteric Modulator PQCA Improves Performance on Translatable Tests of Memory and Attention in Rhesus Monkeys. J Pharmacol Exp Ther. 2015 Dec;355(3):442-50.

[2]. Uslaner JM, et al. The muscarinic M1 receptor positive allosteric modulator PQCA improves cognitive measures in rat, cynomolgus macaque, and rhesus macaque. Psychopharmacology (Berl). 2013 Jan;225(1):21-30.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H20N4O3

[ Molecular Weight ]:
388.41900

[ Exact Mass ]:
388.15400

[ PSA ]:
98.70000

[ LogP ]:
2.38798

Related Compounds

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