A muscarinic M1 receptor antagonist (Ki = 11.48 nM); selective for M1 over M2

Pirenzepine (hydrochloride) – 1 g

Brand:
Cayman
CAS:
29868-97-1
Storage:
-20
UN-No:
Non-Hazardous - /

Pirenzepine is an antagonist of M1 muscarinic acetylcholine receptors (Ki = 11.48 nM).{49496} It is selective for M1 over M2, M3, and M4 receptors (Kis = 602.56, 151.36, and 199.53 nM, respectively). Pirenzepine inhibits ascending reflex contraction of the circular smooth muscle in isolated guinea pig ileal segments induced by intraluminal balloon inflation (IC50 = 501.19 nM). It inhibits methacholine-induced increases in ileal pressure in guinea pigs (ID50 = 724.44 nM). Pirenzepine inhibits oxotremorine-induced gastric ulcer, gastric acid secretion, and salivation in rats (ED50s = 13, 37.5, and 620 μg/kg i.v., respectively).{49497} It prevents form-deprivation myopia (FDM) in a chick model of experimental myopia.{36513}  

 

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Description

A muscarinic M1 receptor antagonist (Ki = 11.48 nM); selective for M1 over M2, M3, and M4 receptors (Kis = 602.56, 151.36, and 199.53 nM, respectively); inhibits ascending reflex contraction of the circular smooth muscle in isolated guinea pig ileal segments induced by intraluminal balloon inflation (IC50 = 501.19 nM); inhibits methacholine-induced increases in ileal pressure in guinea pigs (ID50 = 724.44 nM); inhibits oxotremorine-induced gastric ulcer, gastric acid secretion, and salivation in rats (ED50 = 13, 37.5, and 620 μg/kg i.v., respectively); prevents FDM in a chick model of experimental myopia

Formal name: 5,11-dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, dihydrochloride

Synonyms:  Gastrozepin

Molecular weight: 424.3

CAS: 29868-97-1

Purity: ≥98%

Formulation: A crystalline solid

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