Vernakalant

Names

[ Name ]:
Vernakalant

[Synonym ]:
(3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]-3-pyrrolidinol
(1R,2R)-2-[(3R)-hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)cyclohexane
Kynapid
Vernakalant
3-Pyrrolidinol, 1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]-, (3R)-
Brinavess
(1R-{2R-[2-(3,4-dimethoxyphenyl)-ethoxy]-cyclohex-2-yl})-pyrrolidin-3R-ol
(3R)-1-{(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl}pyrrolidin-3-ol
RSD 1235
(3R)-1-{(1R,2R)-2-[2-(3,4-Dimethoxyphenyl)ethoxy]cyclohexyl}-3-pyrrolidinol
1R-(2R-(2-(3,4-dimethoxy-phenyl)-ethoxy)-cyclohexyl)-pyrrolidin-3R-ol
Vernakalant [INN:BAN]
UNII-9G468C8B13
cc-484
Vernakalant [INN]
(3R)-1-{(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl}pyrrolidinol

Biological Activity

[Description]:

Vernakalant(RSD-1235) is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.IC50 value:Target:

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Research Areas >> Cardiovascular Disease

[References]

[1]. Dorian, Paul MD et al. The Effect of Vernakalant (RSD1235), an Investigational Antiarrhythmic Agent, on Atrial Electrophysiology in Humans. Journal of Cardiovascular Pharmacology:July 2007 - Volume 50 -Issue 1 - pp 35-40.

[2]. Jodene Eldstrom et al. The Molecular Basis of High-Affinity Binding of the Antiarrhythmic Compound Vernakalant (RSD1235) to Kv1.5 Channels. Molecular Pharmacology December 2007 vol. 72 no. 6 1522-1534

[3]. Vernakalant. Too dangerous in atrial fibrillation.Prescrire Int. 2012 May;21(127):119-22.

[4]. Blomstr?m-Lundqvist C, Blomstr?m P.Safety and efficacy of pharmacological cardioversion of atrial fibrillation using intravenous vernakalant, a new antiarrhythmic drug with atrial selectivity.Expert Opin Drug Saf. 2012 Jul;11(4):671-9. Epub 2012 May 26.

[5]. Bash LD, Buono JL, Davies GM, Martin A, Fahrbach K, Phatak H, Avetisyan R, Mwamburi M.Systematic review and meta-analysis of the efficacy of cardioversion by vernakalant and comparators in patients with atrial fibrillation.Cardiovasc Drugs Ther. 2012 Apr;

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
479.0±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₀H₃₁NO₄

[ Molecular Weight ]:
349.464

[ Flash Point ]:
243.5±28.7 °C

[ Exact Mass ]:
349.225311

[ PSA ]:
51.16000

[ LogP ]:
2.40

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.557

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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