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Pirenzepine 2HCl

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Chemical Structure| 29868-97-1 同义名 : Gastrozepin dihydrochloride;Pirenzepin dihydrochloride;Gastrozepin;Pirenzepine (hydrochloride);LS 519;Pirenzepine dihydrochloride
CAS号 : 29868-97-1
货号 : A119911
分子式 : C19H23Cl2N5O2
纯度 : 99+%
分子量 : 424.324
MDL号 : MFCD00055214
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(58.92 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 75 mg/mL(176.75 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Pirenzepine Dihydrochloride is a selective M1 muscarinic receptor antagonist. Pirenzepine (Dihydrochloride) has antisecretory properties on gastric acid and pepsin secretion. Significant cytoprotective properties of pirenzepine have been observed on a variety of experimentally induced peptic ulcerations[3]. In vivo，Pirenzepine (5-25 mg/kg i.v.) also depressed indirect electrical stimulation-evoked twitches of the cat tibialis anterior and soleus muscle preparations[4]. Pirenzepine was 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[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.78mL

2.36mL

1.18mL

23.57mL

4.71mL

2.36mL
参考文献

[1]Daeffler L, Schmidlin F, et al. Inverse agonist activity of pirenzepine at M2 muscarinic acetylcholine receptors. Br J Pharmacol. 1999 Mar;126(5):1246-52.

[2]Eglen RM, Hegde SS, Watson N. Muscarinic receptor subtypes and smooth muscle function. Pharmacol Rev. 1996 Dec;48(4):531-65.

[3]Del Tacca M, Danesi R, Blandizzi C, Bernardini MC. Un antimuscarinico selettivo: la pirenzepina. Rassegna delle sue proprietà farmacologiche e cliniche [A selective antimuscarinic agent: pirenzepine. Review of its pharmacologic and clinical properties]. Minerva Dietol Gastroenterol. 1989 Jul-Sep;35(3):175-89. Italian. PMID: 2574837.

[4]Ojewole JA. Effects of pirenzepine (Gastrozepin) on skeletal muscle contractility. Methods Find Exp Clin Pharmacol. 1983 Nov;5(9):619-23. PMID: 6689440.

[5]Caulfield MP, Higgins GA, Straughan DW. Central administration of the muscarinic receptor subtype-selective antagonist pirenzepine selectively impairs passive avoidance learning in the mouse. J Pharm Pharmacol. 1983 Feb;35(2):131-2. doi: 10.1111/j.2042-7158.1983.tb04290.x. PMID: 6131987.