Pirmenol - CAS 68252-19-7
Category: Inhibitor
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Molecular Formula:
C22H30N2O
Molecular Weight:
338.49
COA:
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Targets:
mAChR
Description:
Pirmenol, also known as CI-845, a new antiarrhythmic drug, inhibits muscarinic acetylcholine receptor-operated K+ current in the guinea pig heart. However, pirmenol has minimal effect on the PR and QRS intervals, and thus does not appear to be a Class IC drug either.
Appearance:
Solid powder
Synonyms:
4-((2R,6S)-2,6-dimethylpiperidin-1-yl)-1-phenyl-1-(pyridin-2-yl)butan-1-ol; Pirmenol.
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
499.6±45.0 °C at 760 Torr
Melting Point:
70-71 °C
Density:
1.046±0.06 g/cm3
Canonical SMILES:
C[C@@H]1CCC[C@@H](N1CCCC(C2=CC=CC=C2)(C3=CC=CC=N3)O)C
1.A patient responding to combined therapy with pirmenol and midodrine for refractory neurally mediated syncope complicated by prostatic hypertrophy.
Mizuguchi Y;Ishimoto T;Kageyama N;Oishi Y;Emi S;Nagase N;Oki T Cardiovasc Drugs Ther. 2004 Sep;18(5):405-8.
A 67-year-old man with neurally mediated syncope (NMS) complicated by prostatic hypertrophy responded well to combined therapy with pirmenol and midodrine. In 2003, syncope occurred while the patient was driving a car. Results of head-up tilt-table testing (HUT) suggested a mixed type of NMS. Oral administration of disopyramide provided severe urinary obstruction. Pirmenol treatment was not associated with syncope during ordinary HUT, but nausea, sweating, and syncope occurred during HUT with provocative administration of isosorbide dinitrate. Combined therapy with pirmenol and midodrine avoided syncope during HUT, and has prevented attacks since discharge from the hospital.
2.A comparison of the binding characteristics of class I antiarrhythmic agents for human muscarinic m1-m3 receptors.
Yamamoto N;Ozaki T;Keida Y;Ohtsuka M;Goto T J Cardiovasc Pharmacol. 1999 Jul;34(1):53-9.
The binding characteristics of the class 1 antiarrhythmic agents, cibenzoline, disopyramide, disopyramide metabolite (the main active metabolite of disopyramide in humans), and pirmenol, for human muscarinic receptors (m1-m3) stably expressed in Chinese hamster ovary cells (CHO) were investigated by binding assay with [3H]N-methylscopolamine ([3H]NMS) as a ligand. All of these agents inhibited the specific [3H]NMS binding to membrane preparations in a concentration-dependent manner. The potencies of affinity of these agents for m1, m2, and m3 receptors (compared by IC50) were disopyramide > pirmenol > disopyramide metabolite > cibenzoline, pirmenol > cibenzoline > disopyramide > disopyramide metabolite, and disopyramide > disopyramide metabolite > pirmenol > cibenzoline, respectively. Some competition curves of cibenzoline, disopyramide, and pirmenol were shallow, and Hill coefficients of these curves differed from unity, suggesting that these agents have allosteric binding characteristics for human muscarinic receptors. The m2-selective ratios to m1 (IC50 m1/IC50 m2) and m3 (IC50 m3/IC50 m2) of cibenzoline were 4.0 and 16, and those of pirmenol were 6.5 and 43, respectively, whereas those of disopyramide and its metabolite ranged from 0.
3.Update on antiarrhythmic drugs in emergency medicine.
Stapczynski JS Emerg Med Clin North Am. 1988 May;6(2):289-315.
Most patients presenting to the Emergency Department with acute arrhythmias can be adequately treated with the available, conventional antiarrhythmics. Recent studies have taught us to use them with better understanding. In the future, several new antiarrhythmics look promising for use in the Emergency Department when given by the intravenous route; particularly, pirmenol, encainide, esmolol, amiodarone, sotalol, and magnesium. However, there have been few comparison studies between various antiarrhythmics, and experience must be gained for a full understanding of the benefits and risks of these agents.
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CAS 68252-19-7 Pirmenol

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