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Chemical Compound Review

Dazodipin     diethyl 2,6-dimethyl-4-(8-oxa-7,9...

Synonyms: DARODIPINE, Darodipino, Dazodipine, Darodipinum, SureCN44696, ...
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Disease relevance of DARODIPINE


Psychiatry related information on DARODIPINE


High impact information on DARODIPINE


Biological context of DARODIPINE


Anatomical context of DARODIPINE


Associations of DARODIPINE with other chemical compounds


Gene context of DARODIPINE

  • Treatment of aged rats with darodipine for 6 months increased the percentage of immunoreactive Purkinje neurons and the intensity of calbindin D-28K immunoreactivity in the cytoplasm of Purkinje neurons [21].
  • Interactions between darodipine or isradipine and the 5-HT1A receptor agonist 8-OHDPAT in rat brain [22].

Analytical, diagnostic and therapeutic context of DARODIPINE

  • In a chronic stroke model (microsphere embolization in rats) PY 108-068 led to a significant reduction in mortality and in the severity of neurological symptoms, whereby the peroral efficacy of the drug could be demonstrated [3].
  • Determination of brain tissue oxygenation with pO2 microelectrodes showed that PY 108-068 improved oxygen supply in the cortex of cats subjected to epicerebral arterial occlusion [3].
  • In a double-blind, randomised crossover study in 6 patients with chronic stable angina, we compared the acute effects of a single oral dose of placebo with 25 mg and 50 mg of PY 108-068 [23].
  • Plasma concentration and CNS effects of Ca antagonists darodipine and nimodipine after single-dose oral administration to healthy volunteers [24].
  • One group was treated with a daily dose of 5 mg/Kg of darodipine, while the control group of SHR was treated with placebo [25].


  1. Objective evaluation of PY-108-068, a new calcium channel inhibitor for the treatment of chronic stable angina pectoris. O'Hara, M.J., Khurmi, N.S., Bowles, M.J., Raftery, E.B. Eur. Heart J. (1985) [Pubmed]
  2. Calcium antagonist (PY 108-068) treatment may further decrease flow in ischemic areas in acute stroke. Vorstrup, S., Andersen, A., Blegvad, N., Paulson, O.B. J. Cereb. Blood Flow Metab. (1986) [Pubmed]
  3. Calcium antagonist PY 108-068: demonstration of its efficacy in various types of experimental brain ischemia. Wiernsperger, N., Gygax, P., Hofmann, A. Stroke (1984) [Pubmed]
  4. Comparison of PY 108-068, a new calcium antagonist, with nifedipine in exercise-induced asthma. Olive, S.R., Hansen, J.E., Sue, D.Y., Ben-Dov, I., Wasserman, K. Chest (1986) [Pubmed]
  5. Effects of the calcium channel antagonist darodipine on ethanol withdrawal in rats. Colombo, G., Agabio, R., Lobina, C., Reali, R., Melis, F., Fadda, F., Gessa, G.L. Alcohol Alcohol. (1995) [Pubmed]
  6. Threshold concentrations of endothelin-1 potentiate contractions to norepinephrine and serotonin in human arteries. A new mechanism of vasospasm? Yang, Z.H., Richard, V., von Segesser, L., Bauer, E., Stulz, P., Turina, M., Lüscher, T.F. Circulation (1990) [Pubmed]
  7. Protective effect of darodipine, a calcium antagonist, on rat cardiomyocytes against oxygen radical-mediated injury. Matucci, R., Ottaviani, M.F., Barbieri, M., Cerbai, E., Mugelli, A. Br. J. Pharmacol. (1997) [Pubmed]
  8. Modification of vasopressin- and angiotensin II- induced changes by calcium antagonists in the peripheral circulation of anaesthetized rabbits. Hof, R.P. Br. J. Pharmacol. (1985) [Pubmed]
  9. Inhibition of myocardial Ca2+ channels by three dihydropyridines with different structural features: potential-dependent blockade by Ro 18-3981. Holck, M., Osterrieder, W. Br. J. Pharmacol. (1987) [Pubmed]
  10. Systemic and regional hemodynamic actions of calcium entry blockers in conscious spontaneously hypertensive rats. Nievelstein, H.M., Van Essen, H., Tijssen, C.M., Smits, J.F., Struyker Boudier, H.A. Eur. J. Pharmacol. (1985) [Pubmed]
  11. The interaction of [3H]PY 108-068 and of [3H]PN 200-110 with calcium channel binding sites in rat brain. Supavilai, P., Karobath, M. J. Neural Transm. (1984) [Pubmed]
  12. Effect of the binding of isradipine and darodipine to different plasma proteins on their transfer through the rat blood-brain barrier. Drug binding to lipoproteins does not limit the transfer of drug. Urien, S., Pinquier, J.L., Paquette, B., Chaumet-Riffaud, P., Kiechel, J.R., Tillement, J.P. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  13. Effect of calcium antagonist darodipine on the isolated human heart. Ginsburg, R., Carey, B., Zera, P. Eur. J. Pharmacol. (1986) [Pubmed]
  14. The effect of dihydropyridine calcium agonists and antagonists on neuronal voltage sensitive calcium channels. Creba, J.A., Karobath, M. Biochem. Biophys. Res. Commun. (1986) [Pubmed]
  15. Effect of treatment with the dihydropyridine-type calcium antagonist darodipine (PY 108-068) on the expression of neurofilament protein immunoreactivity in the cerebellar cortex of aged rats. Vega, J.A., Sabbatini, M., Del Valle, M.E., Amenta, F. Mech. Ageing Dev. (1994) [Pubmed]
  16. Coronary vasodilator compared to cardiac effects of PY 108-068, a new dihydropyridine vasodilator, on isolated, blood-perfused dog-heart preparations. Wada, Y., Satoh, K., Taira, N. J. Cardiovasc. Pharmacol. (1984) [Pubmed]
  17. Cardiovascular effects of two new calcium antagonists, PY 108-068 and PN 200-110, in conscious spontaneously hypertensive rats. Barrès, C., Cerutti, C., Morin, B., Sassard, J. Br. J. Pharmacol. (1988) [Pubmed]
  18. Vasopressin induced myocardial depression in neurally mediated and not due to impaired coronary blood flow. Hof, R.P. Br. J. Pharmacol. (1986) [Pubmed]
  19. The preparation and acute antihypertensive effects of a nanocapsular form of darodipine, a dihydropyridine calcium entry blocker. Hubert, B., Atkinson, J., Guerret, M., Hoffman, M., Devissaguet, J.P., Maincent, P. Pharm. Res. (1991) [Pubmed]
  20. pH dependent binding of ligands to serum lipoproteins. Simon, N., Dailly, E., Jolliet, P., Tillement, J.P., Urien, S. Pharm. Res. (1997) [Pubmed]
  21. Effect of treatment with the dihydropyridine-type calcium antagonist darodipine (PY 108-068) on the expression of calbindin D-28K immunoreactivity in the cerebellar cortex of aged rats. Amenta, F., Mancini, M., Naves, F.J., Vega, J.A., Zaccheo, D. Mech. Ageing Dev. (1995) [Pubmed]
  22. Interactions between darodipine or isradipine and the 5-HT1A receptor agonist 8-OHDPAT in rat brain. Gaggi, R., D'Allolio, R., Santangelo, M., Roncada, P. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  23. PY 108-068--acute effects of a single oral dose in chronic stable angina. de Buitleir, M., Krikler, S., Krikler, D.M. Eur. J. Clin. Pharmacol. (1986) [Pubmed]
  24. Plasma concentration and CNS effects of Ca antagonists darodipine and nimodipine after single-dose oral administration to healthy volunteers. Sannita, W.G., Garbarino, S., Gesino, D., Massimilla, S., Ogliastro, C. Neuropsychobiology (1999) [Pubmed]
  25. Influence of treatment with the calcium channel blocker darodipine (PY 108-068) on the morphology of pial and coronary arteries in spontaneously hypertensive rats. Ferrante, F., Ricci, A., Rossodivita, I., Amenta, F. Clin. Exp. Hypertens. (1994) [Pubmed]
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