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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
Chemical Compound Review

Foridone     dimethyl4-[2- (difluoromethoxy)phenyl]- 2,6...

Synonyms: Foridon, Phoridone, Riodipine, Riodipino, Ryodipine, ...
 
 
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Disease relevance of PP-1466

 

High impact information on PP-1466

  • The results obtained clearly demonstrated that a nontoxic concentration (0.5 microgram/ml) of ryodipine increased (about 5 times) farmarubicin cytotoxicity as the IC50 of the cytostatic was shifted from 1,86 ng/ml on single treatment to 0.37 ng/ml on combined treatment of the cells [3].
  • The effect of ryodipine on calcium outflow from tissues, on contraction force, the duration of action potentials and the relaxation phase time-constant in the contraction cycles of myocardial strips was studied using frog heart preparations [4].
  • Ryodipine (10(-5) mol/l) decreased the relaxation time-constant by about 20% as compared to controls [4].
  • Dependence of Ca outflow and depression of frog myocardium contraction on ryodipine concentration [4].
  • A clear species difference in LD50 values was found in acute toxicity of PP-1466, and rabbits were the most sensitive between animal species used, then dogs, mice and rats in order [1].
 

Biological context of PP-1466

 

Anatomical context of PP-1466

  • The results obtained are as follows: The intraarterial administration of PP-1466 to the femoral artery caused vasodilating response [5].
  • Effect of ryodipine on electromechanical parameters of heart and vessels, cAMP phosphodiesterase activity and swelling-contraction cycle of mitochondria [7].
  • In the isolated rabbit aorta and portal vein PP-1466 is more antagonistic to contractions caused by Ca2+ than by epinephrine [7].
  • 2,6-Dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)-1,4 -dihydropyridine (ryodipine, PP-1466), an effective Ca2+ channel blocker, diminishes contraction force and decreases duration of action potential in the frog heart ventricle strips [7].
 

Associations of PP-1466 with other chemical compounds

  • 2,6-Dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)-1, 4-dihydropyridine (ryodipine, PP-1466) at oral administration in the form of a suspension with Tween (polysorbate) 80 addition is comparatively rapidly absorbed in the gastro-intestinal tract and circulates in blood for a long period of time [6].
 

Analytical, diagnostic and therapeutic context of PP-1466

  • The metabolic fate of [14C]ryosidine (ryodipine) has been investigated after oral administration to human subjects (by capsule), and to rats and dogs (in solution) [8].
  • In rabbits oral PP-1466 decreases in EEG basic rhythm amplitude both in cortical and subcortical structures [2].

References

  1. Acute and subacute toxicity of 2,6-dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)-1 ,4-dihydropyridine (PP-1466). Gomi, T., Yamamoto, H., Ozeki, M., Fujikura, M., Hirao, A., Kobayashi, M., Tateishi, T., Yumoto, S., Okumura, M., Aikawa, K. Arzneimittel-Forschung. (1985) [Pubmed]
  2. Pharmacological and toxicological properties of ryodipine. Kimenis, A.A., Vitolina, R.O., Petersone, I.O., Germane, S.K., Briede, J.L. Arzneimittel-Forschung. (1985) [Pubmed]
  3. Ryodipine-induced enhancement of farmarubicin cytotoxicity against human leukemia cells in vitro. Mircheva, J., Staneva-Stoytcheva, D., Ancheva, M. Acta physiologica et pharmacologica Bulgarica. (1990) [Pubmed]
  4. Dependence of Ca outflow and depression of frog myocardium contraction on ryodipine concentration. Narusevicius, E., Gendviliene, V., Macianskiene, R., Hmelj-Dunai, G., Velena, A., Duburs, G. Gen. Physiol. Biophys. (1988) [Pubmed]
  5. Pharmacological studies of a newly synthetized 1,4-dihydropyridine derivative, 2,6-dimethyl-3,5-dimethoxycarbonyl-4- (o-difluoromethoxyphenyl)-1,4-dihydropyridine (PP-1466). Toribatake, T., Fujii, K., Kobayashi, M., Okumura, M., Aikawa, K. Arzneimittel-Forschung. (1985) [Pubmed]
  6. Pharmacokinetics and metabolism of ryodipine in rats. Parinov, V.J., Odinec, A.G., Gilev, A.P., Dubur, G.J., Muceniece, D.H., Ozol, J.J., Shatz, V.D., Gavars, M.P., Vigante, B.A. Arzneimittel-Forschung. (1985) [Pubmed]
  7. Effect of ryodipine on electromechanical parameters of heart and vessels, cAMP phosphodiesterase activity and swelling-contraction cycle of mitochondria. Velena, A.H., Dubur, G.J., Vitolina, R.O., Kimenis, A.A., Selga, M.J., Zarinsh, G.V., Narusevicius, E.V., Macianskiene, R.A., Gendvilienè, V.I., Simkhovich, B.Z. Arzneimittel-Forschung. (1985) [Pubmed]
  8. Metabolism and pharmacokinetics of the dihydropyridine calcium antagonist, ryosidine, in man. Midgley, I., Chasseaud, L.F., Taylor, I.W., Walmsley, L.M., Fowkes, A.G., Darragh, A., Lambe, R.F., Bonn, R. Xenobiotica (1985) [Pubmed]
 
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