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Pirmenol hydrochloride

Cat. No. M10873
Pirmenol hydrochloride Structure
Synonym:

Cl-845

Size Price Availability
10mg USD 92  USD92 4-7 Days
50mg USD 252  USD252 4-7 Days
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Biological Activity

Pirmenol hydrochloride inhibits IK.ACh (IC50=0.1 μM) by blocking mAchR. Pirmenol hydrochloride can be used in the research of cardiovascular disease. Pirmenol hydrochloride (2.5 and 5 mg/kg, p.o.) is effective against the arrhythmias in conscious, coronary artery ligated dogs.

Chemical Information
Molecular Weight 374.95
Formula C22H31ClN2O
CAS Number 61477-94-9
Solubility (25°C) Water 90 mg/mL
DMSO 100 mg/mL
Storage 4°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] H Atarashi, et al. J Cardiovasc Pharmacol. Clinical effects and pharmacokinetics of a single oral dose of pirmenol hydrochloride

[2] T E Mertz, et al. J Pharmacol Exp Ther. Pirmenol hydrochloride (CI-845) and reference antiarrhythmic agents: effects on early ventricular arrhythmias after acute coronary artery ligation in anesthetized rats

[3] H R Kaplan, et al. Angiology. Pirmenol: preclinical pharmacology

[4] H Kotake, et al. J Electrocardiol. Effects of pirmenol hydrochloride on the spontaneous action potentials and membrane current systems of rabbit sinoatrial node cells

[5] B Reichardt, et al. Naunyn Schmiedebergs Arch Pharmacol. Pirmenol, a new antiarrhythmic drug with potassium- and sodium-channel blocking activity; a voltage-clamp study in rabbit Purkinje fibres

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Keywords: Pirmenol hydrochloride, Cl-845 supplier, AChR/AChE, inhibitors, activators

 
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