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Pirmenol hydrochloride

产品编号 T61529 CAS 61477-94-9

Pirmenol hydrochloride 通过阻断毒蕈碱性受体来抑制IK.ACh。Pirmenol 抑制 Carbachol 诱导的 IK.ACh，IC50值为 0.1 μM。

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Pirmenol hydrochloride Chemical Structure

Pirmenol hydrochloride, CAS 61477-94-9

规格	价格/CNY	货期
2 mg	￥ 269	5日内发货
5 mg	￥ 455	5日内发货
10 mg	￥ 814	5日内发货
1 mL * 10 mM (in DMSO)	￥ 493	5日内发货

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Pirmenol hydrochloride 的其他形式现货产品:

Pirmenol

其他形式的 Pirmenol hydrochloride:

Pirmenol
现货

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生物活性

化学信息

存储 & 溶解度

产品描述	Pirmenol hydrochloride functions by inhibiting I_K.ACh through the blockade of muscarinic receptors, demonstrating a potent effect with an IC_50 value of 0.1 μM for the inhibition of Carbachol-induced I_K.ACh.
体外活性	Pirmenol inhibits the carbachol-induced I K.ACh in a concentration-dependent manner. Pirmenol also inhibits the GTPγS-induced current although the concentrations of Pirmenol needed to inhibit the GTPγS-induced current are much higher than those to inhibit the carbachol-induced I K.ACh. The IC 50 of Pirmenol for inhibition of the GTPγS-induced currents is 30 μM. The inhibitory effect of Pirmenol on these I K.ACh is almost completely reversible and the outward current reappeared upon washout of Pirmenol. Pirmenol on the muscarinic acetylcholine receptor-operated K + current (I K.ACh ) in atrial cells and on experimental atrial fibrillation in isolated guinea-pig hearts. In isolated atrial myocytes, Pirmenol concentration dependently inhibits the I K.ACh induced by carbachol or intracellular loading of GTPγS. In Langendorff-perfused hearts Pirmenol reverses the carbachol-induced decreases in effective refractory periods and atrial fibrillation threshold [1].
体内活性	The pyridine-methanol derivative Pirmenol hydrochloride is a new antiarrhythmic agent. Single-dose studies in rodents demonstrate a 10- to 15-fold difference between the po and iv LD 50 values. In rats, the po LD 50 is 359.9 mg/kg and the iv LD 50 is 23.6 mg/kg. Mice LD 50 values are 215.5 and 20.8 mg/kg for po and iv routes, respectively. Short-term subacute iv toxicity studies in rats (2.5, 5.0, and 7.5 mg/kg) and dogs (2.5, 5, and 10 mg/kg) for 4 weeks elicite minimal reactions. Cardiac effects in dogs include drug related increases in heart rate, increases QRS duration, shortening of ST interval without evidence of cardiac tissue damage and mild local reaction at the injection site. Orally, Pirmenol is well tolerated for 13 weeks in rats receiving 25, 50, and 100 mg/kg/day while dogs given 5, 10, and 15 mg/kg/day shows anticholinergic effects at high levels (dryness of mucosae, body tremors). Heart rates are significantly accelerated only at the beginning of the study and QRS changes are seen with wide individual variations. No drug-related tissue changes are elicited in these species. Teratology studies in rats (50, 100, and 150 mg/kg) and in rabbits (10, 25, and 50 mg/kg) show no overt effect on organogenesis but embryotoxicity is seen at 150 mg/kg in rats [2].

分子量	374.95
分子式	C22H31ClN2O
CAS No.	61477-94-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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对于不同动物的给药剂量换算，您也可以参考 更多...

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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