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1144504-35-7

1144504-35-7 structure
1144504-35-7 structure
  • Name: PQCA
  • Chemical Name: pqca
  • CAS Number: 1144504-35-7
  • Molecular Formula: C22H20N4O3
  • Molecular Weight: 388.41900
  • Catalog: Signaling Pathways GPCR/G Protein mAChR
  • Create Date: 2018-02-17 01:54:56
  • Modify Date: 2024-01-03 14:44:29
  • 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].

Name pqca
Synonyms 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
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
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.

Molecular Formula C22H20N4O3
Molecular Weight 388.41900
Exact Mass 388.15400
PSA 98.70000
LogP 2.38798