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Chemical Compound Review

Sunrythm     N-(2,6-dimethylphenyl)-2- (1,2,3,5,6,7...

Synonyms: SureCN483632, SUN-1165, DU-6552, SUN 1165, LS-139080, ...
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Disease relevance of Pilsicainide

  • Furthermore, the antiarrhythmic action of SUN 1165 in cardiac glycoside-induced arrhythmias in dogs could be mediated not only by an inhibition of sodium channels and subsequent reduction in the intracellular sodium activity, but also by a reduction of intracellular calcium activity due to the Na+-Ca2+ exchange mechanism [1].
  • Administration of SUN 1165 maintained mitochondrial function, and prevented the leakage of lysosomal enzymes caused by ischemia significantly [2].
  • These results indicate that SUN 1165 may selectively inhibit cardiac sodium channels and is likely to be of value in correcting not only ventricular but also supraventricular tachyarrhythmias [3].
  • Dosage adjustment of SUN 1165 is necessary in renal failure [4].
  • In conclusion, SUN-1165 showed antiarrhythmic effects in a canine model of myocardial infarction [5].
 

Psychiatry related information on Pilsicainide

 

High impact information on Pilsicainide

 

Chemical compound and disease context of Pilsicainide

 

Biological context of Pilsicainide

 

Anatomical context of Pilsicainide

 

Associations of Pilsicainide with other chemical compounds

  • Effects of N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate (SUN 1165) on cardiac conduction were studied in anesthetized, anesthetized open-chest and conscious dogs and rabbit Langendorff hearts following either intravenous (i.v.) bolus injection and continuous infusion or intraarterial injection [13].
 

Gene context of Pilsicainide

 

Analytical, diagnostic and therapeutic context of Pilsicainide

  • More than 60% of SUN 1165 given orally was excreted unchanged via the kidney, both by tubular secretion and glomerular filtration [4].
  • The minimum effective concentrations of SUN 1165 for digitalis, 24-h coronary ligation, and 48-h coronary ligation arrhythmias were 0.92 +/- 0.19, 2.5 +/- 0.4, and 1.2 +/- 0.4 micrograms/ml [10].
  • 5. The muscle relaxant effect of SUN 1165 (50%-toxic dose, TD50 = 30 mg/kg p.o.) was more marked than that of lidocaine (TD50 = 92 mg/kg p.o.) on traction test in mice [6].

References

  1. Mechanism of inhibition by SUN 1165, a new Na channel blocking antiarrhythmic agent, of cardiac glycoside-induced triggered activity. Inomata, N., Ishihara, T. Eur. J. Pharmacol. (1988) [Pubmed]
  2. The effects of SUN 1165, a novel sodium channel blocker, on ischemia-induced mitochondrial dysfunction and leakage of lysosomal enzymes in canine hearts. Sugiyama, S., Hanaki, Y., Ogawa, T., Hieda, N., Taki, K., Ozawa, T. Biochem. Biophys. Res. Commun. (1988) [Pubmed]
  3. Electrophysiological actions of N-(2,6-dimethylphenyl)-8-pyrrolizidine-acetamide hydrochloride hemihydrate (SUN 1165), a new antiarrhythmic agent. Hattori, Y., Inomata, N., Aisaka, K., Ishihara, T. J. Cardiovasc. Pharmacol. (1986) [Pubmed]
  4. Pharmacokinetics of SUN 1165, a new antiarrhythmic agent, in renal dysfunction. Takabatake, T., Ohta, H., Yamamoto, Y., Ishida, Y., Hara, H., Ushiogi, Y., Nakamura, S., Hashimoto, N., Sasaki, T., Satoh, S. Eur. J. Clin. Pharmacol. (1991) [Pubmed]
  5. Effects of SUN-1165, N-(2,6-dimethylphenyl)-8-pyrrolizidine acetamide hydrochloride hemihydrate, a new class I antiarrhythmic drug, on ventricular arrhythmias, intraventricular conduction, and the refractory period in canine myocardial infarction. Hashimoto, H., Satoh, N., Nakashima, M. J. Cardiovasc. Pharmacol. (1992) [Pubmed]
  6. General pharmacological studies on N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate. 1st communication: effect on the central nervous system. Hirotsu, I., Kihara, T., Nakamura, S., Hattori, Y., Hatta, M., Kitakaze, Y., Takahama, K., Hashimoto, Y., Miyata, T., Ishihara, T. Arzneimittel-Forschung. (1988) [Pubmed]
  7. Different time courses of the blockade of sodium current by lignocaine and SUN 1165 in single myocytes isolated from guinea-pig atrium. Inomata, N., Ishihara, T., Akaike, N. Br. J. Pharmacol. (1989) [Pubmed]
  8. Effect of SUN 1165, a new potent antiarrhythmic agent, on the kinetics of rate-dependent block of Na channels and ventricular conduction of extrasystoles. Hattori, Y., Hidaka, T., Aisaka, K., Satoh, F., Ishihara, T. J. Cardiovasc. Pharmacol. (1988) [Pubmed]
  9. Effects of N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate on the ventriculo-atrial conductivity of accessory pathways. Satoh, S., Watanabe, J., Keitoku, M., Kinoshita, H., Sekiguchi, N., Endoh, S., Ohtsuka, K., Hangai, K., Morita, M., Takishima, T. Arzneimittel-Forschung. (1989) [Pubmed]
  10. Canine digitalis arrhythmia as a model for detecting Na-channel blocking antiarrhythmic drugs: a comparative study using other canine arrhythmia models and the new antiarrhythmic drugs, propafenone, tocainide, and SUN 1165. Hashimoto, K., Ishii, M., Komori, S., Mitsuhashi, H. Heart and vessels. (1985) [Pubmed]
  11. General pharmacological studies on N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate. 3rd communication: effect on cardiovascular system. Aisaka, K., Hidaka, T., Hattori, Y., Inomata, N., Ishihara, T., Satoh, F. Arzneimittel-Forschung. (1988) [Pubmed]
  12. SUN 1165: a new antiarrhythmic Na current blocker in ventricular myocytes of guinea-pig. Inomata, N., Ishihara, T., Akaike, N. Comp. Biochem. Physiol. C, Comp. Pharmacol. Toxicol. (1987) [Pubmed]
  13. N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate (SUN 1165), a new antiarrhythmic agent: effects on cardiac conduction. Hidaka, T., Hamasaki, S., Aisaka, K., Ishihara, T., Morita, M., Toyama, J., Yamada, K. Arzneimittel-Forschung. (1985) [Pubmed]
  14. General pharmacological studies on N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate. 2nd communication: effect on the peripheral nervous system and peripheral organs. Hirotsu, I., Kihara, T., Hattori, Y., Hatta, M., Hirose, N., Ishihara, T., Satoh, F. Arzneimittel-Forschung. (1988) [Pubmed]
 
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