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Details

Stereochemistry ACHIRAL
Molecular Formula C19H32N2.2ClH
Molecular Weight 361.393
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TEDISAMIL DIHYDROCHLORIDE

SMILES

Cl.Cl.C(C1CC1)N2CC3CN(CC4CC4)CC(C2)C35CCCC5

InChI

InChIKey=NXXZICGFHYJPGE-UHFFFAOYSA-N
InChI=1S/C19H32N2.2ClH/c1-2-8-19(7-1)17-11-20(9-15-3-4-15)12-18(19)14-21(13-17)10-16-5-6-16;;/h15-18H,1-14H2;2*1H

HIDE SMILES / InChI

Molecular Formula C19H32N2
Molecular Weight 288.4708
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Tedisamil is an antiarrhythmic with additional anti-ischaemic properties, which acts via potassium channel blockade. This drug can be categorised as a class III antiarrhythmic agent due to its effects of action potential and QT interval prolongation in these patients. Although tedisamil has been shown to be an effective anti-ischaemic agent, with Phase III trials for angina pectoris now completed, the company are now pursuing the use of tedisamil for the treatment of atrial fibrillation, for which tedisamil is still in Phase II/III clinical trials. The FDA’s Cardiovascular and Renal Drugs Advisory Committee voted not to recommend approval for Solvay Pharmaceuticals’ investigational anti-arrhythmic drug Pulzium (Tedisamil) and asked the company to give the FDA more information.

Approval Year

PubMed

PubMed

TitleDatePubMed
Genomic organization, chromosomal localization, tissue distribution, and biophysical characterization of a novel mammalian Shaker-related voltage-gated potassium channel, Kv1.7.
1998 Mar 6
Dispersion of cell-to-cell uncoupling precedes low K+-induced ventricular fibrillation.
2001
Tedisamil and dofetilide-induced torsades de pointes, rate and potassium dependence.
2001 Apr
Tedisamil (Solvay).
2001 Jan
Tedisamil: master switch of nature?
2001 Jan
Effects of tedisamil on cardiovascular tissues isolated from normo- and hypertensive rats.
2001 Jul
Transgenic mice overexpressing human KvLQT1 dominant-negative isoform. Part II: Pharmacological profile.
2001 May
Newer antiarrhythmic drugs.
2001 May-Jun
Conversion of atrial fibrillation by the experimental antiarrhythmic drug tedisamil in two canine models.
2001 Oct
New antiarrhythmic drugs for the treatment of atrial fibrillation.
2002 Feb
Tedisamil blocks BK-type Ca(2+)-dependent K(+) channels and modulates action potentials in rat hippocampal neurons.
2002 Feb 15
Bertosamil blocks HERG potassium channels in their open and inactivated states.
2002 Sep
Tedisamil and lidocaine enhance each other's antiarrhythmic activity against ischaemia-induced arrhythmias in rats.
2003 Aug
Modulation of intracellular Ca(2+) concentration by tedisamil, a class III antiarrhythmic agent, in isolated heart preparation.
2003 Aug 22
Tedisamil in coronary disease: additional benefits in the therapy of atrial fibrillation?
2003 Jun
Antiarrhythmic drug therapy of atrial fibrillation: focus on new agents.
2003 Jun
Atrial fibrillation: emerging possibilities for drug treatment: an overview of current opportunities and recent developments.
2003 Jun
Role of atrial fibrillation threshold evaluation on guiding treatment.
2003 Oct 1
Trials of new antiarrhythmic drugs for maintenance of sinus rhythm in patients with atrial fibrillation.
2004
Trial finds new anti-arrhythmic, tedisamil, is superior to placebo for converting recent onset atrial fibrillation or atrial flutter.
2004 Dec
Effect of the antifibrillatory compound tedisamil (KC-8857) on transmembrane currents in mammalian ventricular myocytes.
2004 Dec
Tedisamil: a new novel antiarrhythmic.
2004 Feb
Theoretical possibilities for the development of novel antiarrhythmic drugs.
2004 Jan
Role of pharmacotherapy in Brugada syndrome.
2004 Jan 1
Safety and efficacy of intravenously administered tedisamil for rapid conversion of recent-onset atrial fibrillation or atrial flutter.
2004 Jul 7
Tedisamil attenuates foetal transformation of myosin in the hypertrophied rat myocardium.
2004 Nov
Electrical storms in Brugada syndrome: review of pharmacologic and ablative therapeutic options.
2005 Jan 1
Do we need pharmacological therapy for atrial fibrillation in the ablation era?
2006 Dec
Approach to the asymptomatic patients with Brugada syndrome.
2007 Apr 1
New antiarrhythmic treatment of atrial fibrillation.
2007 Jul
Relationship among amiodarone, new class III antiarrhythmics, miscellaneous agents and acquired long QT syndrome.
2008
Update on atrial fibrillation: part II.
2008 Mar
New horizons in antiarrhythmic therapy: will novel agents overcome current deficits?
2008 Sep 22
Recent advances in pharmacotherapy of atrial fibrillation.
2009 Aug
Novel antiarrhythmic drugs in atrial fibrillation: focus on tedisamil.
2009 Aug
The transmembrane beta-subunits KCNE1, KCNE2, and DPP6 modify pharmacological effects of the antiarrhythmic agent tedisamil on the transient outward current Ito.
2009 Jun
Clinically important interaction between tedisamil and verapamil.
2009 May
Atrial fibrillation: from ion channels to bedside treatment options.
2009 Nov-Dec

Sample Use Guides

The recommended dose is 0.32 mg/kg
Route of Administration: Intravenous
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:29:48 GMT 2023
Edited
by admin
on Fri Dec 15 15:29:48 GMT 2023
Record UNII
S5O682VL3K
Record Status Validated (UNII)
Record Version
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Name Type Language
TEDISAMIL DIHYDROCHLORIDE
MI  
Common Name English
TEDISAMIL DIHYDROCHLORIDE [MI]
Common Name English
KC-8857 DIHYDROCHLORIDE
Code English
SPIRO(CYCLOPENTANE-1,9'-(3,7)DIAZABICYCLO(3.3.1)NONANE), 3',7'-BIS(CYCLOPROPYLMETHYL)-, HYDROCHLORIDE (1:2)
Common Name English
Code System Code Type Description
CAS
132523-84-3
Created by admin on Fri Dec 15 15:29:48 GMT 2023 , Edited by admin on Fri Dec 15 15:29:48 GMT 2023
PRIMARY
PUBCHEM
11566690
Created by admin on Fri Dec 15 15:29:48 GMT 2023 , Edited by admin on Fri Dec 15 15:29:48 GMT 2023
PRIMARY
FDA UNII
S5O682VL3K
Created by admin on Fri Dec 15 15:29:48 GMT 2023 , Edited by admin on Fri Dec 15 15:29:48 GMT 2023
PRIMARY
MERCK INDEX
m10516
Created by admin on Fri Dec 15 15:29:48 GMT 2023 , Edited by admin on Fri Dec 15 15:29:48 GMT 2023
PRIMARY Merck Index
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