Name | pirenzepine dihydrochloride |
Synonyms | Tabe Leblon Maghen Ulcosan Renzepin Gasteril Ulcuforton Pirenzepine HCL PIRENZEPINE HCL HYDRATE pirenzepine hydrochloride pirenzepine dihydrochloride 11-[2-(4-methylpiperazin-1-yl)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one hydrate hydrochloride 11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride 5,11-Dihydro-11-((4-methylpiperazin-1-yl)acetyl)-6H-pyrido(2,3-b)-(1,4)benzodiazepin-6-one dihydrochloride 5,11-dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-β][1,4]benzo- diazepin-6-one Dihydrochloride |
CAS | 29868-97-1 |
EINECS | 249-907-5 |
InChI | InChI=1/C19H21N5O2.ClH.H2O/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);1H;1H2 |
Molecular Formula | C19H23Cl2N5O2 |
Molar Mass | 424.32 |
Melting Point | 248-250°C |
Solubility | H2O: 50mg/mL |
Appearance | powder |
Color | white |
Storage Condition | Inert atmosphere,2-8°C |
Sensitive | Hygroscopic |
MDL | MFCD00055214 |
Use | For the treatment of gastric and duodenal ulcer, acute gastric mucosal bleeding and other diseases |
In vitro study | The antisecretory properties of pirenzepine on gastric acid and pepsin secretion may be attributed to the antagonistic activity of the drug on muscarinic M1 receptors of gastric intramural plexuses, whereas the effect on parietal muscarinic M2 receptors seems of less importance. Additional inhibitory mechanisms on gastric secretion may be represented by pirenzepine-induced increase in somatostatin release from gastrointestinal system. Significant cytoprotective properties of pirenzepinehave been observed on a variety of experimentally induced peptic ulcerations. Pirenzepine (5-500 μg/mL) inhibits agonist-(acetylcholine-, carbachol- or nicotine-) induced contractions of the toad isolated rectus abdominis muscle, and depresses electrically provoked twitches of the rat phrenic nerve-hemidiaphragm muscle preparation. |
In vivo study | Pirenzepine is potent in impairing learning of an avoidance; much higher doses are required to antagonize other central muscarinic effects. Pirenzepine is found to impair passive avoidance learning when given i.c.v. 20 min pre-training. The median latencies in pirenzepine-treated animals are 79.5, 11, 27 and 25.5 seconds with doses of 0.03, 0.1, 0.3 and 1 μg per mouse respectively. Acid and pepsin secretion stimulated by either bethanechol or the vagus are inhibited in a dose-responsive manner by pirenzepine. Pirenzepine (5-25 mg/kg i.v.) depresses indirect electrical stimulation-evoked twitches of the cat tibialis anterior and soleus muscle preparations. |
WGK Germany | 2 |
RTECS | UU7883000 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.357 ml | 11.784 ml | 23.567 ml |
5 mM | 0.471 ml | 2.357 ml | 4.713 ml |
10 mM | 0.236 ml | 1.178 ml | 2.357 ml |
5 mM | 0.047 ml | 0.236 ml | 0.471 ml |