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Chemical Compound Review

Tocris-1123     3-(4,4-diphenyl-1- piperidyl)propyl methyl...

Synonyms: Tocris-1124, CHEMBL41929, CHEMBL405355, SureCN245992, CHEBI:159934, ...
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High impact information on NIGULDIPINE

  • The chemotherapeutic effect of B859-35, the (-)-enantiomer of dihydropyrine 3-methyl-5-3-(4,4-diphenyl-1-piperidinyl)-propyl-1,4-dihydro-2,6-dimethy l-4- (3-nitrophenyl)-pyridine-3,5-dicarboxylate-hydrochloride (niguldipine), was tested on tumors induced in Syrian golden hamsters by N-nitrosodiethylamine (DEN) [1].
  • Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine [2].
  • Yohimbine decreased the dose of convulsant needed to produce tonic hindlimb extension, while niguldipine enhanced doses of picrotoxin needed to produce both symptoms [3].
  • 4. The (-)- and (+)-enantiomers of niguldipine had an equal and low affinity for alpha 1-adrenoceptor binding sites both in untreated (log Ki-6.66 and -6.90 respectively) and CEC-treated membranes in which approximately 70% of sites had been inactivated (log Ki-6.41 and -6.86 respectively) [4].
  • Niguldipine discriminates between alpha 1-adrenoceptor-mediated second messenger responses in rat cerebral cortex slices [5].

Biological context of NIGULDIPINE


Anatomical context of NIGULDIPINE


Associations of NIGULDIPINE with other chemical compounds

  • The biological activity of the (+)-S- and (-)-R-enantiomers of niguldipine, of the (-)-S- and (+)-R-enantiomers of felodipine and nitrendipine, and of rac-nisoldipine and rac-nimodipine was investigated in vitro and in vivo [11].

Gene context of NIGULDIPINE

  • These compounds were designed to maximize inhibition of P-glycoprotein and minimize calcium channel binding activity, based on structure modifications of niguldipine [12].
  • A series of 4-aryl-1,4-dihydropyridines and corresponding aromatized 4-arylpyridines have been synthesized based on structure modifications of niguldipine to enhance multidrug resistance reversal activity, while minimizing calcium channel binding [13].

Analytical, diagnostic and therapeutic context of NIGULDIPINE

  • They were voltage-clamped with a single patch electrode technique (whole cell recording) in order to analyse the effects of niguldipine on ionic membrane currents [6].
  • A simple and reliable reversed-phase high-performance liquid chromatography method was developed and validated for the determination of DHP-014, a niguldipine analogue with potent P-glycoprotein inhibitory and negligible calcium channel blocking properties, in rat plasma [14].


  1. Successful chemotherapy of experimental neuroendocrine lung tumors in hamsters with an antagonist of Ca2+/calmodulin. Schuller, H.M., Correa, E., Orloff, M., Reznik, G.K. Cancer Res. (1990) [Pubmed]
  2. Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. Wetzel, J.M., Miao, S.W., Forray, C., Borden, L.A., Branchek, T.A., Gluchowski, C. J. Med. Chem. (1995) [Pubmed]
  3. The involvement of alpha2-adrenoceptors in the anticonvulsive effect of swim stress in mice. Pericić, D., Svob, D., Jazvinsćak Jembrek, M., Mirković Kos, K. Psychopharmacology (Berl.) (2001) [Pubmed]
  4. Rat pineal alpha 1-adrenoceptor subtypes: studies using radioligand binding and reverse transcription-polymerase chain reaction analysis. Sugden, D., Anwar, N., Klein, D.C. Br. J. Pharmacol. (1996) [Pubmed]
  5. Niguldipine discriminates between alpha 1-adrenoceptor-mediated second messenger responses in rat cerebral cortex slices. Robinson, J.P., Kendall, D.A. Br. J. Pharmacol. (1990) [Pubmed]
  6. The dihydropyridine niguldipine modulates calcium and potassium currents in vascular smooth muscle cells. Klöckner, U., Isenberg, G. Br. J. Pharmacol. (1989) [Pubmed]
  7. Cardiac alpha(1)-adrenoceptors that regulate contractile function: subtypes and subcellular signal transduction mechanisms. Endoh, M. Neurochem. Res. (1996) [Pubmed]
  8. Effects of niguldipine, a new dihydropyridine calcium antagonist, on regional blood flow, cardiac performance and myocardial metabolism in anaesthetized open-chest dogs. Fischer, G., Schneider, W., Krumpl, G., Grohs, J.G., Raberger, G. Archives internationales de pharmacodynamie et de thérapie. (1989) [Pubmed]
  9. Stereoselectivity of Ca2+ channel block by dihydropyridines: no modulation by the voltage protocol. Handrock, R., Herzig, S. Eur. J. Pharmacol. (1996) [Pubmed]
  10. Age-related changes in Ca2+ channel antagonist receptors in rabbit lower urinary tract. Yoshida, M., Latifpour, J., Weiss, R.M. Eur. J. Pharmacol. (1993) [Pubmed]
  11. Stereoselective inhibition of thromboxane-induced coronary vasoconstriction by 1,4-dihydropyridine calcium channel antagonists. Eltze, M., Boer, R., Sanders, K.H., Boss, H., Ulrich, W.R., Flockerzi, D. Chirality. (1990) [Pubmed]
  12. Effects of new 4-aryl-1,4-dihydropyridines and 4-arylpyridines on drug efflux mediated by multidrug resistance-associated protein 1. Zhou, X.F., Coburn, R.A., Morris, M.E. Journal of pharmaceutical sciences. (2005) [Pubmed]
  13. New 4-aryl-1,4-dihydropyridines and 4-arylpyridines as P-glycoprotein inhibitors. Zhou, X.F., Zhang, L., Tseng, E., Scott-Ramsay, E., Schentag, J.J., Coburn, R.A., Morris, M.E. Drug Metab. Dispos. (2005) [Pubmed]
  14. A high-performance liquid chromatographic method for determination of the niguldipine analogue DHP-014. Zhou, X.F., Wang, Q., Coburn, R.A., Morris, M.E. Biomed. Chromatogr. (2006) [Pubmed]
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