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盐酸哌仑西平 /Pirenzepine 2HCl {[allProObj[0].p_purity_real_show]}

货号:A119911 同义名: Gastrozepin dihydrochloride;Pirenzepin dihydrochloride Ambeed 开学季,买赠积分,赢豪礼

Pirenzepine 2HCl is a is an anticholinergic agent and induces the dimerization of muscarinic M1 receptors, used to treat myopia, gastric and duodenal ulcers.

Pirenzepine 2HCl 化学结构 CAS号:29868-97-1
Pirenzepine 2HCl 化学结构
CAS号:29868-97-1
Pirenzepine 2HCl 3D分子结构
CAS号:29868-97-1
Pirenzepine 2HCl 化学结构 CAS号:29868-97-1
Pirenzepine 2HCl 3D分子结构 CAS号:29868-97-1
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Pirenzepine 2HCl 纯度/质量文件 产品仅供科研

货号:A119911 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 nM

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Loganin ++

AChE, IC50: 3.95 μM

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topride HCl ++

AChE, IC50: 2.04 μM

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Dehydroevodiamine HCl {[allProObj[0].p_purity_real_show]}
Jatrorrhizine ++

AChE, IC50: 872 nM

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Palmatine ++

AChE, IC50: 0.51 μM

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(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

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Galanthamine HBr ++

AChE, IC50: 0.35 μM

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Trospium chloride {[allProObj[0].p_purity_real_show]}
Tiotropium Bromide Monohydrate {[allProObj[0].p_purity_real_show]}
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

{[allProObj[0].p_purity_real_show]}
Hexamethonium Bromide {[allProObj[0].p_purity_real_show]}
Pancuronium dibromide {[allProObj[0].p_purity_real_show]}
Neostigmine bromide {[allProObj[0].p_purity_real_show]}
Orphenadrine citrate {[allProObj[0].p_purity_real_show]}
Oxybutynin {[allProObj[0].p_purity_real_show]}
Irsogladine PDE {[allProObj[0].p_purity_real_show]}
Pyridostigmine bromide {[allProObj[0].p_purity_real_show]}
Rivastigmine +

AChR, IC50: 5.5 μM

{[allProObj[0].p_purity_real_show]}
Paroxetine hydrochloride {[allProObj[0].p_purity_real_show]}
Rocuronium Bromide {[allProObj[0].p_purity_real_show]}
Tropicamide +++

M4 mAChR, IC50: 8 nM

{[allProObj[0].p_purity_real_show]}
Diphenmanil methylsulfate {[allProObj[0].p_purity_real_show]}
Umeclidinium bromide {[allProObj[0].p_purity_real_show]}
Otilonium bromide {[allProObj[0].p_purity_real_show]}
Flavoxate HCl +

mAChR, IC50: 12.2 μM

{[allProObj[0].p_purity_real_show]}
Ipratropium bromide {[allProObj[0].p_purity_real_show]}
Diphenidol HCl {[allProObj[0].p_purity_real_show]}
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

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Aclidinium Bromide ++++

M2 mAChR, Ki: 0.1 nM

M4 mAChR, Ki: 0.21 nM

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Oxybutynin chloride {[allProObj[0].p_purity_real_show]}
Pentoxyverine citrate {[allProObj[0].p_purity_real_show]}
Solifenacin {[allProObj[0].p_purity_real_show]}
Catharanthine {[allProObj[0].p_purity_real_show]}
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

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Vinblastine sulfate +

nAChR, IC50: 8.9 μM

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PNU-120596 ++

α7 nAChR, EC50: 216 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Pirenzepine 2HCl 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].

Pirenzepine 2HCl 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.

Pirenzepine 2HCl 实验方案

计算器
存储液制备 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

Pirenzepine 2HCl 技术信息

CAS号29868-97-1
分子式C19H23Cl2N5O2
分子量 424.324
别名 Gastrozepin dihydrochloride;Pirenzepin dihydrochloride;Gastrozepin;Pirenzepine (hydrochloride);LS 519;Pirenzepine dihydrochloride
运输蓝冰
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
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