Chemical Property of hydron;11-[2-(4-methylpiperazin-1-yl)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one;chloride
Chemical Property:
- Appearance/Colour:white powder
- Melting Point:248-250 °C
- Boiling Point:541.7 °C at 760 mmHg
- Flash Point:281.4 °C
- PSA：74.23000
- Density:g/cm3
- LogP:2.80740
- Storage Temp.:-20?C Freezer
- Sensitive.:Hygroscopic
- Solubility.:H2O: 50 mg/mL
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:2
- Exact Mass:387.1462027
- Heavy Atom Count:27
- Complexity:534
- Purity/Quality:
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99% *data from raw suppliers
Pirenzepine, Dihydrochloride *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:[H+].CN1CCN(CC1)CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4.[Cl-]
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Description
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.
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Uses
An antiulcerative. Tricyclic gastric-acid inhibitor. Antiulcerative;M1 antagonist
