| Bioactivity | 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[1][2][4]. |
| Target | IC50: 0.1 μM (IK.ACh) |
| Invitro | Pirmenol (1 μM) hydrochloride inhibits the IK.ACh induced by carbachol or intracellular loading of GTPg S in in atrial cells[1].Pirmenol (5 μM) hydrochloride depresses the early part of the plateau and lengthened the final repolarization of the action potentials in ventricular myocytes[3].Pirmenol (1 μM) hydrochloride prolongs the action potential duration at 90% repolarization in atrial muscles and Purkinje fibers[3]. |
| In Vivo | Pirmenol (2.5 and 5 mg/kg, p.o.) hydrochloride is effective against the arrhythmias in conscious, coronary artery ligated dogs[4].Pirmenol (rats) hydrochloride shows LD50s of 359.9 mg/kg (p.o), 23.6 mg/kg (i.v.)[2].Pirmenol (mice) hydrochloride shows LD50s of 215.5 mg/kg (p.o), 20.8 mg/kg (i.v.)[2]. Animal Model: |
| Name | Pirmenol hydrochloride |
| CAS | 61477-94-9 |
| Formula | C22H31ClN2O |
| Molar Mass | 374.95 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [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. |
Pirmenol hydrochloride
CAS: 61477-94-9 F: C22H31ClN2O W: 374.95
Pirmenol ((±)-Pirmenol) hydrochloride is an orally active antiarrhythmic agent. Pirmenol hydrochloride inhibits IK.ACh
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