Pirmenol hydrochloride

(Synonyms: 盐酸吡美诺; (±)-Pirmenol hydrochloride; CI-845)
目录号: PL06854 纯度: ≥99%
Pirmenol ((±)-Pirmenol) hydrochloride 是一种具有口服活性的抗心律失常剂。Pirmenol hydrochloride 通过阻断毒蕈碱性受体 (mAchR) 来抑制 IK.ACh (IC50: 0.1 μM)。Pirmenol hydrochloride 可用于心血管疾病的研究,如心房颤动。
CAS No. :61477-94-9
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中文名称
Pirmenol hydrochloride
中文别名
4-[(2R,6s)-2,6-二甲基-1-哌啶]-1-苯基-1-吡啶-2-丁烷-1-醇盐酸盐;吡美诺;盐酸吡美诺;4-[(2R,6S)-2,6-dimethyl-1-piperidyl]-1-phenyl-1-pyridin-2-yl-butan-1-o l hydrochloride
英文名称
Pirmenol hydrochloride
英文别名
4-((2R,6S)-2,6-Dimethylpiperidin-1-yl)-1-phenyl-1-(pyridin-2-yl)butan-1-ol hydrochloride;4-[(2R,6S)-2,6-dimethyl-1-piperidyl]-1-phenyl-1-pyridin-2-yl-butan-1-o l hydrochloride;4-[(2S,6R)-2,6-dimethylpiperidin-1-yl]-1-phenyl-1-pyridin-2-ylbutan-1-ol,hydrochloride;PIRMENOL HYDROCHLORIDE;(±)-Pirmenol hydrochloride;4-[(2R,6S)-2,6-dimethylpiperidin-1-yl]-1-phenyl-1-pyridin-2-ylbutan-1-ol hydrochloride;CCRIS 5234;CI 845;Cl-845;Pirmenol HCl;Pirmenol hydrochloride (USAN);Pirmenol hydrochloride [USAN];Pirmenol hydrochloride monohydrate;Pirmenol.HCl;Pirmenol hydrochloride
Cas No.
61477-94-9
分子式
C22H30N2O.HCl
分子量
374.95
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
详情描述
Pirmenol ((±)-Pirmenol) hydrochloride 是一种具有口服活性的抗心律失常剂。Pirmenol hydrochloride 通过阻断毒蕈碱性受体 (mAchR) 来抑制 IK.ACh (IC50: 0.1 μM)。Pirmenol hydrochloride 可用于心血管疾病的研究,如心房颤动。
产品详情
Pirmenol ((±)-Pirmenol) hydrochloride 是一种具有口服活性的抗心律失常剂。Pirmenol hydrochloride 通过阻断毒蕈碱性受体 (mAchR) 来抑制 IK.ACh (IC50: 0.1 μM)。Pirmenol hydrochloride 可用于心血管疾病的研究,如心房颤动。
生物活性
Pirmenol ((±)-Pirmenol) hydrochloride is an orally active antiarrhythmic agent. Pirmenol hydrochloride inhibits I K.ACh (IC 50 : 0.1 μM) by blocking mAchR. Pirmenol hydrochloride can be used in the research of cardiovascular disease, such as atrial fibrillation.
性状
Solid
IC50 & Target[1][2]
IC50: 0.1 μM (IK.ACh)
体外研究(In Vitro)
Pirmenol (1 μM) hydrochloride inhibits the IK.ACh induced by carbachol or intracellular loading of GTPg S in in atrial cells.
Pirmenol (5 μM) hydrochloride depresses the early part of the plateau and lengthened the final repolarization of the action potentials in ventricular myocytes.
Pirmenol (1 μM) hydrochloride prolongs the action potential duration at 90% repolarization in atrial muscles and Purkinje fibers.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Pirmenol (2.5 and 5 mg/kg, p.o.) hydrochloride is effective against the arrhythmias in conscious, coronary artery ligated dogs.
Pirmenol (rats) hydrochloride shows LD 50 s of 359.9 mg/kg (p.o), 23.6 mg/kg (i.v.).
Pirmenol (mice) hydrochloride shows LD 50 s of 215.5 mg/kg (p.o), 20.8 mg/kg (i.v.).
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Watanabe Y, et al. Pirmenol inhibits muscarinic acetylcholine receptor-operated K+ current in the guinea pig heart. Eur J Pharmacol. 1997 Oct 29;338(1):71-4.
[2]. Schardein JL, et al. Preclinical toxicology studies with a new antiarrhythmic agent: Pirmenol hydrochloride (CI-845). Toxicol Appl Pharmacol. 1980 Nov;56(2):294-301.
溶解度数据
In Vitro: DMSO : 125 mg/mL (333.38 mM; Need ultrasonic)H2O : 100 mg/mL (266.70 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Watanabe Y, et al. Pirmenol inhibits muscarinic acetylcholine receptor-operated K+ current in the guinea pig heart. Eur J Pharmacol. 1997 Oct 29;338(1):71-4.
[2]. Schardein JL, et al. Preclinical toxicology studies with a new antiarrhythmic agent: Pirmenol hydrochloride (CI-845). Toxicol Appl Pharmacol. 1980 Nov;56(2):294-301.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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