| 产品描述: | Pirmenol ((±)-Pirmenol) hydrochloride is an orally active antiarrhythmic agent. Pirmenol hydrochloride inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol hydrochloride can be used in the research of cardiovascular disease, such as atrial fibrillation |
| 靶点: |
IC50: 0.1 μM (IK.ACh) |
| 体内研究: |
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 LD50s of 359.9 mg/kg (p.o), 23.6 mg/kg (i.v.). Pirmenol (mice) hydrochloride shows LD50s of 215.5 mg/kg (p.o), 20.8 mg/kg (i.v.) Animal Model: Conscious, coronary artery ligated dogs Dosage: Oral administration (p.o.) Administration: 2.5 and 5 mg/kg Result: Restored normal sinus rhythm, and showed a long duration of activity, wide safety margin. |
| 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. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
RT |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.667 ml |
13.335 ml |
26.67 ml |
| 5 mM |
0.533 ml |
2.667 ml |
5.334 ml |
| 10 mM |
0.267 ml |
1.334 ml |
2.667 ml |
| 50 mM |
0.053 ml |
0.267 ml |
0.533 ml |
|
| 注意: |
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