| 产品描述: | Pirmenol 是一种具有口服活性的抗心律失常剂。Pirmenol 通过阻断毒蕈碱性受体 (mAchR) 来抑制 IK.ACh (IC50: 0.1 μM)。可用于心血管疾病的研究,如心房颤动。Pirmenol 通过阻断毒蕈碱性受体 (mAchR) 来抑制 IK.ACh (IC50: 0.1 μM)。Pirmenol 可用于心血管疾病的研究,如心房颤动。 |
| 靶点: |
IC50: 0.1 μM (IK.ACh) |
| 体外研究: |
Pirmenol (1 μM) inhibits the IK.ACh induced by carbachol or intracellular loading of GTPg S in in atrial cells. Pirmenol (5 μM) depresses the early part of the plateau and lengthened the final repolarization of the action potentials in ventricular myocytes. Pirmenol (1 μM) prolongs the action potential duration at 90% repolarization in atrial muscles and Purkinje fibers. |
| 体内研究: |
Pirmenol (2.5 and 5 mg/kg, p.o.) is effective against the arrhythmias in conscious, coronary artery ligated dogs. Pirmenol (rats) shows LD50s of 359.9 mg/kg (p.o), 23.6 mg/kg (i.v.). Pirmenol (mice) shows LD50s of 215.5 mg/kg (p.o), 20.8 mg/kg (i.v.). |
| 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.
3. T Sawanobori, et al. Electrophysiologic and antiarrhythmic actions of pirmenol on rabbit and guinea pig cardiac preparations. J Cardiovasc Pharmacol. 1990 Dec;16(6):975-83.
4. T E Mertz, et al. Pirmenol hydrochloride (CI-845): antiarrhythmic profile in coronary artery ligated conscious dogs. J Cardiovasc Pharmacol. 1980 Sep-Oct;2(5):527-41. |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.954 ml |
14.771 ml |
29.543 ml |
| 5 mM |
0.591 ml |
2.954 ml |
5.909 ml |
| 10 mM |
0.295 ml |
1.477 ml |
2.954 ml |
| 50 mM |
0.059 ml |
0.295 ml |
0.591 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |