PQCA - CAS 1144504-35-7
Catalog number: 1144504-35-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C22H20N4O3
Molecular Weight:
388.43
COA:
Inquire
Targets:
mAChR
Description:
This active molecular is a muscarinic M1 receptor positive allosteric modulator which is able to improve cognitive measures in rat and rhesus monkeys. PQCA is very efficient in rodent and nonhuman primate (NHP) cognition assays and it can improve performance on translatable tests of Memory and Attention in rhesus monkeys. PQCA attenuates learning and memory deficits in Alzheimer's disease model. PQCA may be potential useful in treating Alzheimer's diseases in the future.
Purity:
98%
Appearance:
POWDER
Synonyms:
1-((4-cyano-4-(pyridin-2-yl)piperidin-1-yl)methyl)-4-oxo-4H-quinolizine-3-carboxylic acid,1401512-98-8 (sodium)
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
treatment of Alzheimer's diseases
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams.
Canonical SMILES:
O=C(C1=CC(CN2CCC(C3=NC=CC=C3)(C#N)CC2)=C4C=CC=CN4C1=O)O
1.Evidence for Classical Cholinergic Toxicity Associated with Selective Activation of M1 Muscarinic Receptors.
Alt A;Pendri A;Bertekap RL Jr;Li G;Benitex Y;Nophsker M;Rockwell KL;Burford NT;Sum CS;Chen J;Herbst JJ;Ferrante M;Hendricson A;Cvijic ME;Westphal RS;O'Connell J;Banks M;Zhang L;Gentles RG;Jenkins S;Loy J;Macor JE J Pharmacol Exp Ther. 2016 Feb;356(2):293-304. doi: 10.1124/jpet.115.226910. Epub 2015 Nov 18.
The muscarinic acetylcholine receptor subtype 1 (M1) receptors play an important role in cognition and memory, and are considered to be attractive targets for the development of novel medications to treat cognitive impairments seen in schizophrenia and Alzheimer's disease. Indeed, the M1 agonist xanomeline has been shown to produce beneficial cognitive effects in both Alzheimer's disease and schizophrenia patients. Unfortunately, the therapeutic utility of xanomeline was limited by cholinergic side effects (sweating, salivation, gastrointestinal distress), which are believed to result from nonselective activation of other muscarinic receptor subtypes such as M2 and M3. Therefore, drug discovery efforts targeting the M1 receptor have focused on the discovery of compounds with improved selectivity profiles. Recently, allosteric M1 receptor ligands have been described, which exhibit excellent selectivity for M1 over other muscarinic receptor subtypes. In the current study, the following three compounds with mixed agonist/positive allosteric modulator activities that are highly functionally selective for the M1 receptor were tested in rats, dogs, and cynomologous monkeys: (3-((1S,2S)-2-hydrocyclohexyl)-6-((6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)methyl)benzo[h]quinazolin-4(3H)-one; 1-((4-cyano-4-(pyridin-2-yl)piperidin-1-yl)methyl)-4-oxo-4H-quinolizine-3-carboxylic acid; and (R)-ethyl 3-(2-methylbenzamido)-[1,4'-bipiperidine]-1'-carboxylate).
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CAS 1144504-35-7 PQCA

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