Pirenzepine (hydrochloride)

Pirenzepine is an antagonist of M1 muscarinic acetylcholine receptors (Ki = 11.48 nM). 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 nmol/kg). Pirenzepine inhibits oxotremorine-induced gastric ulcer, gastric acid secretion, and salivation in rats (ED50s = 13, 37.5, and 620 µg/kg i.v., respectively). It prevents form-deprivation myopia (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. CAS Number: 29868-97-1. Synonyms: Gastrozepin. Molecular Formula: C19H21N5O2 . 2HCl. Formula Weight: 424.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 10 mg/ml. lambdamax: 280 nm. SMILES: O=C1NC2=C(N=CC=C2)N(C(CN3CCN(C)CC3)=O)C4=C1C=CC=C4.Cl.Cl. InChi Code: InChI=1S/C19H21N5O2.2ClH/c1-22-9-11-23(12-10-22)13-17(25)24-16-7-3-2-5-14(16)19(26)21-15-6-4-8-20-18(15)24,,/h2-8H,9-13H2,1H3,(H,21,26),2*1H. InChi Key: FFNMBRCFFADNAO-UHFFFAOYSA-N.