Dronedarone hydrochloride

Modify Date: 2024-01-03 08:18:26

Dronedarone hydrochloride Structure
Dronedarone hydrochloride structure
Common Name Dronedarone hydrochloride
CAS Number 141625-93-6 Molecular Weight 593.217
Density N/A Boiling Point 683.9ºC at 760mmHg
Molecular Formula C31H45ClN2O5S Melting Point NA (low-melting)
MSDS Chinese USA Flash Point 367.4ºC

 Use of Dronedarone hydrochloride


Dronedarone hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.

 Names

Name Dronedarone Hydrochloride
Synonym More Synonyms

 Dronedarone hydrochloride Biological Activity

Description Dronedarone hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
Related Catalog
In Vitro Dronedarone (SR-33589) is a multichannel blocker for atrial fibrillation . It is a potent inhibitor of the acetylcholine-activated K+ current from atrial and sinoatrial nodal tissue, and inhibits the rapid delayed rectifier more potently than slow and inward rectifier K+ currents and inhibits L-type calcium current. Under whole-cell patch clamp, it blocks IKr (IC50=3 μM) and ICa-L (IC50=0.18 μM). The effects on ICa-L are use- and frequency-dependent. Dronedarone inhibits current carried by human ether-a-go-go gene (HERG)-expressing oocytes (analagous to IKr) with an IC50 of 9 μM[1]. In guinea pig ventricular myocytes, dronedarone exhibits a state dependent inhibition of the fast Na+ channel current with an IC50 of 0.7±0.1 μM, when the holding potential is −80 mV[2].
In Vivo Dronedarone (Hydrochloride) reduces significantly the incidence of ventricular fibrillation (VF) from 80 to 30% (p < 0.05) at 3 mg/kg i.v. and eliminated VF and mortality at 10 mg/kg i.v. [3]. Dronedarone inhibited carotid artery thrombus formation in vivo. Thrombin- and collagen-induced platelet aggregation is impaired indronedarone-treated mice (P\0.05), and expression ofplasminogen activator inhibitor-1 (PAI1), an inhibitor of the fibrinolytic system, is reduced in the arterial wall[4].
Animal Admin Rats: Rats are anesthetized, artificially ventilated, and the thorax opened by a left thoracotomy. Ischemia is induced by left coronary artery ligation, and reperfusion is achieved (after a 5-min period of ischemia) in a separate group of rats by removing the ligature. Agents are given intravenously 5 min before occlusion or orally 4 h before study[3]. Mice: Twelve-week-old C57Bl/6 mice are divided into two groups: dronedarone (200 mg/kg body weight with a once daily oral gavage for 14 days) or control (1.4 % methylcellulose). Twenty-four hours after the last application, mice are anesthetized by intraperitoneal injection of 87 mg/kg sodium pentobarbital. Rose bengal is diluted to 12 mg/mL in phosphate-buffered saline and then injected into the tail vein at a concentration of 63 mg/kg[4].
References

[1]. Bogdan R, et al. Effect of?dronedarone?on Na+, Ca2+ and HCN channels. Naunyn Schmiedebergs Arch Pharmacol.?2011 Apr;383(4):347-56.?

[2]. Doggrell SA, et al. Dronedarone: an amiodarone analogue. Expert Opin Investig Drugs. 2004 Apr;13(4):415-26.

[3]. Manning AS, et al. SR 33589, a new amiodarone-like agent: effect on ischemia- and reperfusion-induced arrhythmias in anesthetized rats. J Cardiovasc Pharmacol. 1995 Sep;26(3):453-61.

[4]. Breitenstein A, et al. Dronedarone reduces arterial thrombus formation. Basic Res Cardiol. 2012 Nov;107(6):302.

 Chemical & Physical Properties

Boiling Point 683.9ºC at 760mmHg
Melting Point NA (low-melting)
Molecular Formula C31H45ClN2O5S
Molecular Weight 593.217
Flash Point 367.4ºC
Exact Mass 592.273743
PSA 97.23000
LogP 9.00480
Appearance of Characters white to off-white
Vapour Pressure 1.47E-18mmHg at 25°C
Storage condition Refrigerator
Water Solubility DMSO: soluble15mg/mL, clear

 Safety Information

RIDADR UN 3077 9 / PGIII

 Articles2

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Inactivation of Human Cytochrome P450 3A4 and 3A5 by Dronedarone and N-Desbutyl Dronedarone.

Mol. Pharmacol. 89 , 1-13, (2015)

Dronedarone is an antiarrhythmic agent approved in 2009 for the treatment of atrial fibrillation. An in-house preliminary study demonstrated that dronedarone inhibits cytochrome P450 (CYP) 3A4 and 3A5...

 Synonyms

n-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)methanesulfonamide monohydrochloride
N-(2-Butyl-3-{4-[3-(dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl)methanesulfonamide hydrochloride (1:1)
Methanesulfonamide, N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5-benzofuranyl]-, hydrochloride (1:1)
Multaq Hydrochloride.
Methanesulfonamide, N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)-, monohydrochloride
Multaq
Dronedarone (Hydrochloride)
Dronedarone hydrochloride
Dronedarone HCl
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