The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
Chemical Compound Review

Almoklant     4-[3-(ethyl-(3- propylsulfinylpropyl)amino)...

Synonyms: Almokalant, Almokalantum, AC1MHWND, AGN-PC-003LTN, CHEMBL362103, ...
 
 
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.
 

Disease relevance of Almokalantum

 

High impact information on Almokalantum

 

Chemical compound and disease context of Almokalantum

 

Biological context of Almokalantum

  • The electropharmacologic effects and pharmacokinetics of almokalant, a new class III antiarrhythmic, were investigated in a randomized, placebo-controlled, double-blind study, and efficacy was evaluated [4].
  • The ability of various human derived in vitro systems to predict various aspects of the in vivo metabolism and kinetics of almokalant have been investigated in a multicenter collaborative study [11].
  • The class III antiarrhythmic drug almokalant (ALM) was given to pregnant rats on Gestation Day 11 (125 micromol/kg) or 13 (25 micromol/kg) [12].
  • Positive inotropism due to lengthening of the cardiac repolarization (almokalant) is considered as class IV action [13].
  • We studied the haemodynamic and metabolic effects of the novel class III antiarrhythmic agent almokalant (H 234/09) in acute ischaemic heart failure at a dose prolonging ventricular repolarization [14].
 

Anatomical context of Almokalantum

 

Associations of Almokalantum with other chemical compounds

 

Gene context of Almokalantum

 

Analytical, diagnostic and therapeutic context of Almokalantum

  • Spontaneous TdP was observed in 9 of 14 dogs after almokalant and could be increased to 12 of 14 with programmed electrical stimulation [1].
  • Almokalant in a dose of 250 nmol/kg i.v., significantly decreased the incidence of reperfusion induced ventricular fibrillation (21% vs. 75% in the control group) and increased the proportion of surviving animals during reperfusion (86% vs. 42%) [25].
  • The four isomers of almokalant, a new antiarrhythmic substance under investigation, were separated by liquid chromatography on a Chiralcel OD and a Chiralpak AD column containing cellulose and amylose tris(3,5-dimethylphenylcarbamate), respectively [26].
  • METHODS: The electrophysiological effects of a 6-hour infusion of almokalant, to a total dose of 25 +/- 4 mg, were assessed by ECG and transesophageal atrial electrograms (TAE) in 100 consecutive patients with atrial fibrillation/flutter (n = 95/5) of 8 +/- 12 months' duration (range 1 to 99 months) [27].
  • Almokalant, a recently developed potassium-channel blocker, has exhibited properties of a selective class III agent in vitro and in animal experiments [15].

References

  1. Further observations to elucidate the role of interventricular dispersion of repolarization and early afterdepolarizations in the genesis of acquired torsade de pointes arrhythmias: a comparison between almokalant and d-sotalol using the dog as its own control. Verduyn, S.C., Vos, M.A., van der Zande, J., Kulcsàr, A., Wellens, H.J. J. Am. Coll. Cardiol. (1997) [Pubmed]
  2. Proarrhythmic effects of the class III agent almokalant: importance of infusion rate, QT dispersion, and early afterdepolarisations. Carlsson, L., Abrahamsson, C., Andersson, B., Duker, G., Schiller-Linhardt, G. Cardiovasc. Res. (1993) [Pubmed]
  3. Attenuation of proarrhythmias related to delayed repolarization by low-dose lidocaine in the anesthetized rabbit. Carlsson, L., Drews, L., Duker, G., Schiller-Linhardt, G. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  4. Electropharmacologic effects and pharmacokinetics of almokalant, a new class III antiarrhythmic, in patients with healed or healing myocardial infarcts and complex ventricular arrhythmias. Wiesfeld, A.C., Crijns, H.J., Tobé, T.J., Almgren, O., Bergstrand, R.H., Aberg, J., Haaksma, J., Lie, K.I. Am. J. Cardiol. (1992) [Pubmed]
  5. Cellular basis of biventricular hypertrophy and arrhythmogenesis in dogs with chronic complete atrioventricular block and acquired torsade de pointes. Volders, P.G., Sipido, K.R., Vos, M.A., Kulcsár, A., Verduyn, S.C., Wellens, H.J. Circulation (1998) [Pubmed]
  6. Potassium and calcium current blocking properties of the novel antiarrhythmic agent H 345/52: implications for proarrhythmic potential. Amos, G.J., Abrahamsson, C., Duker, G., Hondeghem, L., Palmer, M., Carlsson, L. Cardiovasc. Res. (2001) [Pubmed]
  7. Effects of E-4031, almokalant and tedisamil on postrest action potential duration of human papillary muscles. Ohler, A., Ravens, U. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  8. Rhythm anomalies related to delayed repolarization in vivo: influence of sarcolemmal Ca++ entry and intracellular Ca++ overload. Carlsson, L., Drews, L., Duker, G. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  9. Proarrhythmic effects of intravenous quinidine, amiodarone, D-sotalol, and almokalant in the anesthetized rabbit model of torsade de pointes. Farkas, A., Leprán, I., Papp, J.G. J. Cardiovasc. Pharmacol. (2002) [Pubmed]
  10. Prevention of class III-induced proarrhythmias by flecainide in an animal model of the acquired long QT syndrome. Hallman, K., Carlsson, L. Pharmacol. Toxicol. (1995) [Pubmed]
  11. An assessment of human liver-derived in vitro systems to predict the in vivo metabolism and clearance of almokalant. Andersson, T.B., Sjöberg, H., Hoffmann, K.J., Boobis, A.R., Watts, P., Edwards, R.J., Lake, B.G., Price, R.J., Renwick, A.B., Gómez-Lechón, M.J., Castell, J.V., Ingelman-Sundberg, M., Hidestrand, M., Goldfarb, P.S., Lewis, D.F., Corcos, L., Guillouzo, A., Taavitsainen, P., Pelkonen, O. Drug Metab. Dispos. (2001) [Pubmed]
  12. Teratogenicity of the class III antiarrhythmic drug almokalant. Role of hypoxia and reactive oxygen species. Wellfelt, K., Sköld, A.C., Wallin, A., Danielsson, B.R. Reprod. Toxicol. (1999) [Pubmed]
  13. Classification of positive inotropic actions based on electrophysiologic characteristics: where should calcium sensitizers be placed? Varro, A., Papp, J.G. J. Cardiovasc. Pharmacol. (1995) [Pubmed]
  14. Class III antiarrhythmic action and inotropy: effects of almokalant in acute ischaemic heart failure in dogs. Mortensen, E., Yang, T., Refsum, H. Pharmacol. Toxicol. (1992) [Pubmed]
  15. Selective Ik blocker almokalant exhibits class III--specific effects on the repolarization and refractoriness of the human heart: a study of healthy volunteers using right ventricular monophasic action potential recordings. Darpö, B., Vallin, H., Almgren, O., Bergstrand, R., Insulander, P., Edvardsson, N. J. Cardiovasc. Pharmacol. (1995) [Pubmed]
  16. Prolonged action potential duration and positive inotropy induced by the novel class III antiarrhythmic agent H 234/09 (Almokalant) in isolated human ventricular muscle. Carlsson, L., Abrahamsson, C., Almgren, O., Lundberg, C., Duker, G. J. Cardiovasc. Pharmacol. (1991) [Pubmed]
  17. Stage-specific skeletal and visceral defects of the I(Kr)-blocker almokalant: further evidence for teratogenicity via a hypoxia-related mechanism. Sköld, A.C., Wellfelt, K., Danielsson, B.R. Teratology (2001) [Pubmed]
  18. Three thiadiazinone derivatives, EMD 60417, EMD 66430, and EMD 66398, with class III antiarrhythmic activity but different electrophysiologic profiles. Himmel, H.M., Wettwer, E., Lues, I., Beier, N., Jonas, R., Ravens, U. J. Cardiovasc. Pharmacol. (2001) [Pubmed]
  19. Differential effects of the new class III antiarrhythmic agents almokalant, E-4031 and D-sotalol, and of quinidine, on delayed rectifier currents in guinea pig ventricular myocytes. Wettwer, E., Grundke, M., Ravens, U. Cardiovasc. Res. (1992) [Pubmed]
  20. Lidocaine and nisoldipine attenuate almokalant-induced dispersion of repolarization and early afterdepolarizations in vitro. Abrahamsson, C., Carlsson, L., Duker, G. J. Cardiovasc. Electrophysiol. (1996) [Pubmed]
  21. Block of HERG-carried K+ currents by the new repolarization delaying agent H 345/52. Amos, G.J., Jacobson, I., Duker, G., Carlsson, L. J. Cardiovasc. Electrophysiol. (2003) [Pubmed]
  22. Frequency-dependent effects of 4-aminopyridine and almokalant on action-potential duration of adult and neonatal rabbit ventricular muscle. Elizalde, A., Barajas, H., Navarro-Polanco, R., Sánchez-Chapula, J. J. Cardiovasc. Pharmacol. (1999) [Pubmed]
  23. Almokalant glucuronidation in human liver and kidney microsomes: evidence for the involvement of UGT1A9 and 2B7. Gaiser, B.K., Lockley, D.J., Staines, A.G., Baarnhielm, C., Burchell, B. Xenobiotica (2003) [Pubmed]
  24. Developmental toxicity of the class III antiarrhythmic agent almokalant in mice. Adverse effects mediated via induction of embryonic heart rhythm abnormalities. Sköld, A.C., Danielsson, B.R. Arzneimittel-Forschung. (2000) [Pubmed]
  25. Comparison of the antiarrhythmic and the proarrhythmic effect of almokalant in anaesthetised rabbits. Farkas, A., Leprán, I., Papp, J.G. Eur. J. Pharmacol. (1998) [Pubmed]
  26. Direct chiral separation of almokalant on Chiralcel OD and Chiralpak AD for liquid chromatographic assay of biological samples. Balmeŕ, K., Lagerström, P.O., Larsson, S., Persson, B.A. J. Chromatogr. (1993) [Pubmed]
  27. Effects of the Ikr-blocker almokalant and predictors of conversion of chronic atrial tachyarrhythmias to sinus rhythm. A prospective study. Houltz, B., Darpö, B., Swedberg, K., Blomström, P., Brachmann, J., Crijns, H.J., Jensen, S.M., Svernhage, E., Vallin, H., Edvardsson, N. Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy. (1999) [Pubmed]
 
WikiGenes - Universities