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Chemical Compound Review

nisoldipine     2-methylpropyl methyl 2,6-dimethyl-4-(2...

Synonyms: Zadipina, Baymycard, Nisocor, Nisoldipin, Syscor, ...
 
 
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Disease relevance of Bay k 5552

 

Psychiatry related information on Bay k 5552

  • Patients in the moderate therapy group were given placebo, while the patients randomized to intensive therapy received either nisoldipine or enalapril in a blinded manner as the initial antihypertensive medication [6].
  • 5. In conclusion nisoldipine, as well as other calcium antagonists, may have a place in the treatment of some mood disorders [7].
 

High impact information on Bay k 5552

 

Chemical compound and disease context of Bay k 5552

  • This response was inhibited by hirudin and nisoldipine, but not by propranolol, prazosin, or pretreatment with pertussis toxin [9].
  • Group III hearts were pretreated with nisoldipine (1 microgram/min) for 5 minutes before ischemia, and group IV hearts were treated with nitroglycerin (93 micrograms/min) before and after ischemia to mimic the vasodilation caused by nisoldipine [10].
  • In 12 rats bearing Walker 256 carcinomas i.p. injection of 0.2-0.4 mg/kg nisoldipine caused a reduction in the tumor-to-muscle flow relationship of 4.4 +/- 1.9 (SD) to 1.74 +/- 0.86 as determined by intraarterial 133Xe injection; i.p. injection of 2-8 mg/kg 5-HT (N = 13) caused a respective reduction from 3.9 +/- 2.67 to 1.3 +/- 1.59 [11].
  • Albuminuria was reduced 47% (95% CI 21-65) in the lisinopril group versus an increase of 11% (-3 to 27) in the nisoldipine group (P = 0.001) [12].
  • The effects of the addition of slow-release nifedipine 20 mg twice daily and nisoldipine 10 mg twice daily to atenolol monotherapy were compared in a double-blind placebo-controlled study of 24 patients with chronic stable angina pectoris [13].
 

Biological context of Bay k 5552

 

Anatomical context of Bay k 5552

  • Single nisoldipine-sensitive calcium channels in smooth muscle cells isolated from rabbit mesenteric artery [17].
  • Thus, in the conscious baboon, nisoldipine administered 1 hour after coronary artery occlusion exerted a marked effect in diminishing reperfusion-induced arrhythmias and improved blood flow to the ischemic zone during occlusion but did not salvage ischemic tissue [16].
  • This study was designed to afford direct viewing of the effects of myocardial ischemia-reperfusion on the coronary microcirculation and to determine whether pretreatment with the calcium blocker nisoldipine would attenuate any microvascular damage during reperfusion [10].
  • Nifedipine and nisoldipine blocked bag cell Ca2+ currents with effects similar to those seen previously on Ca2+ currents in cardiac muscle: both compounds appeared to interact with Ca2+ channels when they were closed, open, and inactivated [18].
  • We thus conclude that the more potent nisoldipine inhibition of smooth muscle versus cardiac L-type Ca2+ channels is not attributable to differences in channel inactivation or activation [19].
 

Associations of Bay k 5552 with other chemical compounds

 

Gene context of Bay k 5552

 

Analytical, diagnostic and therapeutic context of Bay k 5552

  • Nisoldipine significantly accelerated the decline in [Ca2+]i during reperfusion and improved recovery of contractility and relaxation [3].
  • Nisoldipine or placebo was administered twice daily for 4 weeks and symptom-limited exercise tests were repeated at 2 and 10-14 hours after the double-blind medication [4].
  • The experimental group of animals (n = 7) was treated with the calcium channel blocker nisoldipine (0.1 microgram/kg/min) from 1 hour after coronary occlusion to 3 hours after coronary reperfusion [16].
  • The effects of nisoldipine on regional myocardial perfusion and neuro-hormonal status were assessed in a double-blind, placebo-controlled study of 32 patients [29].
  • Nisoldipine was administered as a 4.5 micrograms kg-1 intravenous bolus over 3 min followed by intravenous infusion of 0.2 microgram kg-1 min-1 during 60 min [30].

References

  1. The effect of nisoldipine as compared with enalapril on cardiovascular outcomes in patients with non-insulin-dependent diabetes and hypertension. Estacio, R.O., Jeffers, B.W., Hiatt, W.R., Biggerstaff, S.L., Gifford, N., Schrier, R.W. N. Engl. J. Med. (1998) [Pubmed]
  2. Nisoldipine and myocardial infarction. Gheorghiade, M. N. Engl. J. Med. (1998) [Pubmed]
  3. Intracellular calcium and ventricular function. Effects of nisoldipine on global ischemia in the isovolumic, coronary-perfused heart. Amende, I., Bentivegna, L.A., Zeind, A.J., Wenzlaff, P., Grossman, W., Morgan, J.P. J. Clin. Invest. (1992) [Pubmed]
  4. Double-blind, dose-response, placebo-controlled multicenter study of nisoldipine. A new second-generation calcium channel blocker in angina pectoris. Thadani, U., Zellner, S.R., Glasser, S., Bittar, N., Montoro, R., Miller, A.B., Chaitman, B., Schulman, P., Stahl, A., DiBianco, R. Circulation (1991) [Pubmed]
  5. Hemodynamic mechanisms of antianginal action of calcium channel blocker nisoldipine in dynamic exercise-induced angina. Yokota, M., Miyahara, T., Iwase, M., Watanabe, M., Matsunami, T., Kamihara, S., Koide, M., Saito, H., Takeuchi, J. Circulation (1990) [Pubmed]
  6. Effects of aggressive blood pressure control in normotensive type 2 diabetic patients on albuminuria, retinopathy and strokes. Schrier, R.W., Estacio, R.O., Esler, A., Mehler, P. Kidney Int. (2002) [Pubmed]
  7. Comparison among the effects of nifedipine, nimodipine and nisoldipine on the brain biogenic amines of normal or haloperidol treated rats. Gaggi, R., Cont, R., Gianni, A.M. Gen. Pharmacol. (1993) [Pubmed]
  8. Evidence for an essential role of reactive oxygen species in the genesis of late preconditioning against myocardial stunning in conscious pigs. Sun, J.Z., Tang, X.L., Park, S.W., Qiu, Y., Turrens, J.F., Bolli, R. J. Clin. Invest. (1996) [Pubmed]
  9. Thrombin modulates phosphoinositide metabolism, cytosolic calcium, and impulse initiation in the heart. Steinberg, S.F., Robinson, R.B., Lieberman, H.B., Stern, D.M., Rosen, M.R. Circ. Res. (1991) [Pubmed]
  10. Prevention of transcoronary macromolecular leakage after ischemia-reperfusion by the calcium entry blocker nisoldipine. Direct observations in isolated rat hearts. McDonagh, P.F., Roberts, D.J. Circ. Res. (1986) [Pubmed]
  11. Increased thermal response to ultrasound in the Walker carcinosarcoma treated with vasoactive drugs. Knapp, W.H., Debatin, J., Helus, F., Sinn, H.J., Ostertag, H. Cancer Res. (1989) [Pubmed]
  12. Differences between nisoldipine and lisinopril on glomerular filtration rates and albuminuria in hypertensive IDDM patients with diabetic nephropathy during the first year of treatment. Rossing, P., Tarnow, L., Boelskifte, S., Jensen, B.R., Nielsen, F.S., Parving, H.H. Diabetes (1997) [Pubmed]
  13. A comparison of nisoldipine and nifedipine, in combination with atenolol, in the management of myocardial ischaemia. Donaldson, K.M., Dawkins, K.D., Waller, D.G. Eur. Heart J. (1993) [Pubmed]
  14. A dihydropyridine (Bay k 8644) that enhances calcium currents in guinea pig and calf myocardial cells. A new type of positive inotropic agent. Thomas, G., Chung, M., Cohen, C.J. Circ. Res. (1985) [Pubmed]
  15. Mechanism of Ca++ antagonist-induced vasodilation. Intracellular actions. Saida, K., van Breemen, C. Circ. Res. (1983) [Pubmed]
  16. Effects of calcium channel blocker on responses of blood flow, function, arrhythmias, and extent of infarction following reperfusion in conscious baboons. Vatner, S.F., Patrick, T.A., Knight, D.R., Manders, W.T., Fallon, J.T. Circ. Res. (1988) [Pubmed]
  17. Single nisoldipine-sensitive calcium channels in smooth muscle cells isolated from rabbit mesenteric artery. Worley, J.F., Deitmer, J.W., Nelson, M.T. Proc. Natl. Acad. Sci. U.S.A. (1986) [Pubmed]
  18. Blockade of Ca2+ and K+ currents in bag cell neurons of Aplysia californica by dihydropyridine Ca2+ antagonists. Nerbonne, J.M., Gurney, A.M. J. Neurosci. (1987) [Pubmed]
  19. Isoform-specific inhibition of L-type calcium channels by dihydropyridines is independent of isoform-specific gating properties. Hu, H., Marban, E. Mol. Pharmacol. (1998) [Pubmed]
  20. Effects of a chronic treatment by nisoldipine, a calcium antagonistic dihydropyridine, on arteries of spontaneously hypertensive rats. Godfraind, T., Kazda, S., Wibo, M. Circ. Res. (1991) [Pubmed]
  21. Alternans of action potential duration after abrupt shortening of cycle length: differences between dog Purkinje and ventricular muscle fibers. Saitoh, H., Bailey, J.C., Surawicz, B. Circ. Res. (1988) [Pubmed]
  22. NFAT4 movement in native smooth muscle. A role for differential Ca(2+) signaling. Stevenson, A.S., Gomez, M.F., Hill-Eubanks, D.C., Nelson, M.T. J. Biol. Chem. (2001) [Pubmed]
  23. Appropriate Blood Pressure Control in NIDDM (ABCD) Trial. Schrier, R.W., Estacio, R.O., Jeffers, B. Diabetologia (1996) [Pubmed]
  24. Effects of calcium channel blockers on pial vascular responses to receptor mediated constrictors. Rosenblum, W.I. Stroke (1984) [Pubmed]
  25. Effects of calcium- and ETA-receptor antagonists on endothelin-induced vasoconstriction and levels of endothelin in the human internal mammary artery. Liu, J.J., Casley, D., Wojta, J., Gallicchio, M., Dauer, R., Johnston, C.I., Buxton, B.F. Clin. Exp. Pharmacol. Physiol. (1994) [Pubmed]
  26. Effects of nisoldipine on endothelin-1- and angiotensin II-induced immediate/early gene expression and protein synthesis in adult rat ventricular cardiomyocytes. Grohé, C., Nouskas, J., Vetter, H., Neyses, L. J. Cardiovasc. Pharmacol. (1994) [Pubmed]
  27. Telmisartan improves insulin sensitivity in nondiabetic patients with essential hypertension. Benndorf, R.A., Rudolph, T., Appel, D., Schwedhelm, E., Maas, R., Schulze, F., Silberhorn, E., Böger, R.H. Metab. Clin. Exp. (2006) [Pubmed]
  28. Prophylactic effects of m-nisoldipine and nisoldipine on reperfusion arrhythmias exacerbated by free radical generating system in Langendorff heart of rat. Li, Y.L., Fu, S.X., Li, Y.S. Zhongguo yao li xue bao = Acta pharmacologica Sinica. (1989) [Pubmed]
  29. Effects of nisoldipine therapy on myocardial perfusion and neuro-hormonal status in patients with severe ischaemic left ventricular dysfunction. Rousseau, M.F., Melin, J., Benedict, C.R., Ahn, S., Raphaël, D., Bornemann, M., Pouleur, H. Eur. Heart J. (1994) [Pubmed]
  30. The acute effects of intravenous nisoldipine on left ventricular function within 24 h after acute myocardial infarction. Chin, J.C., van der Wall, E.E., Manger Cats, V., van der Laarse, A., Blokland, J.A., Pauwels, E.J., Bruschke, A.V. Eur. Heart J. (1992) [Pubmed]
 
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