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Chemical Compound Review

FOSTEDIL     2-[4- (diethoxyphosphorylmethyl) phenyl]benz...

Synonyms: Fosfedil, Fostedilum, CHEMBL39516, KB-944, Abbott 53986, ...
 
 
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Disease relevance of Fosfedil

 

Psychiatry related information on Fosfedil

 

High impact information on Fosfedil

 

Biological context of Fosfedil

  • Depression by KB-944 of SA nodal automaticity and AV nodal conduction occurred pari passu with coronary vasodilation, whereas force of contraction was depressed to a lesser extent in coronary vasodilator doses [4].
  • The doses of KB-944 leading to a decrease in systolic blood pressure of 20% of pretreatment level were estimated to be 32.8 mg/kg in normotensive rats, 5.1 mg/kg in SHR, 6.4 mg/kg in renal hypertensive rats and 5.4 mg/kg in DOCA-NaCl hypertensive rats, respectively [5].
  • Effects of a new calcium entry blocking agent, KB-944, on the membrane potential and currents of mammalian ventricular muscle cells [6].
  • Neither death nor inhibition of body weight gain nor any toxic symptoms of the drug were noted in rats but an increase in water intake was found in the rats treated with over 100 mg/kg/day of KB-944 [7].
  • The method consisted of mutagens or KB-944 with and without metabolic activation, and two bacteria; Salmonella typhimurium 5 test strains, TA 1535, TA 100, TA 1537, TA 1538 and TA 98, and Escherichia coli WP 2 uvr A [8].
 

Associations of Fosfedil with other chemical compounds

 

Analytical, diagnostic and therapeutic context of Fosfedil

  • Thus, KB-944 maintains ischemic zone blood flow despite decreases in coronary perfusion pressure and increases in tissue flow in the collateral dependent region when aortic pressure is prevented from decreasing [1].
  • Ambulatory monitoring and multistage treadmill exercise with computer-assisted electrocardiographic analysis was performed after 2 weeks of placebo therapy and after two 2-weekly periods of KB-944 therapy [3].
  • The anti-anginal effects of KB-944 (Fostedil), a new calcium ion antagonist with a half life of approximately 23-28 hr, were evaluated in 20 patients with exertional angina pectoris in a placebo-controlled single-blind dose titration trial [3].
  • In SHR, tolerance of KB-944 was not observed with oral administration for 5 weeks at a daily dose of 30 mg/kg [5].

References

  1. Effects of KB-944, a novel calcium antagonist, in several models of canine myocardial ischemia. Pelc, L.R., Gross, G.J., Warltier, D.C. J. Pharmacol. Exp. Ther. (1986) [Pubmed]
  2. The effects of calcium entry blockade on the vulnerability of infarcted canine myocardium toward ventricular fibrillation. Lynch, J.J., Montgomery, D.G., Lucchesi, B.R. J. Pharmacol. Exp. Ther. (1986) [Pubmed]
  3. Ambulatory monitoring and exercise testing in the evaluation of a new long-acting calcium ion antagonist KB-944 (Fostedil) for the treatment of exertional angina pectoris. Khurmi, N.S., Bowles, M.J., O'Hara, M.J., Lahiri, A., Raftery, E.B. International journal of cardiology. (1985) [Pubmed]
  4. Cardiac versus coronary vasodilator actions of KB-944, a new calcium antagonist, assessed in isolated, blood-perfused heart preparations of dogs. Taira, N., Kawada, M., Satoh, K. J. Cardiovasc. Pharmacol. (1983) [Pubmed]
  5. Antihypertensive effect of KB-944, a new calcium antagonist, in conscious normotensive and hypertensive rats. Morita, T., Kanazawa, T., Ito, K., Nose, T. Arzneimittel-Forschung. (1982) [Pubmed]
  6. Effects of a new calcium entry blocking agent, KB-944, on the membrane potential and currents of mammalian ventricular muscle cells. Iijima, T., Morita, T., Taira, N. Archives internationales de pharmacodynamie et de thérapie. (1985) [Pubmed]
  7. 1-month subacute oral toxicity study of KB-944, a new calcium antagonist, in rats. Hirakawa, K., Unno, T., Ogino, F., Takebe, H., Iino, T., Nose, T. Arzneimittel-Forschung. (1982) [Pubmed]
  8. Mutagenicity evaluation of KB-944, a new calcium antagonist, in the Ames bacterial system. Tanaka, H., Tanaka, A., Tsunetoshi, Y., Sotomura, M., Nose, T. Arzneimittel-Forschung. (1982) [Pubmed]
  9. Vasodilator action of KB-944, a new calcium antagonist. Morita, T., Yoshino, K., Kanazawa, T., Ito, K., Nose, T. Arzneimittel-Forschung. (1982) [Pubmed]
  10. Vasodilator mechanism of KB-944, a new calcium antagonist. Morita, T., Kanazawa, T., Ito, K., Nose, T. Arzneimittel-Forschung. (1982) [Pubmed]
 
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