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Chemical Compound Review

Lercanil     [1-(3,3-diphenylpropyl- methyl-amino)-2...

Synonyms: masnidipine, Lercanidipine, Lercanil (TN), SureCN25268, CHEMBL250270, ...
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Disease relevance of Lercanidipine


High impact information on Lercanidipine


Chemical compound and disease context of Lercanidipine


Biological context of Lercanidipine

  • There was no clinically relevant reduction in clinic or ambulatory blood pressure with 2.5 mg lercanidipine, and the effect was superimposable on that of placebo [8].
  • The method can be used to quantify lercanidipine in human plasma covering a variety of pharmacokinetic or bioequivalence studies [14].
  • Lercanidipine had the lowest negative inotropic efficacy (1 micromol/L LER: 60.3% basal < AML: 79.1% basal < NIF: 92.4 basal) and potency (IC50 NIF: 3.5 nmol/L < AML: 48 nmol/L < Ler: 127 nmol/L) in right atrial trabeculae [15].
  • Therefore, we demonstrate for the first time that lercanidipine consistently decreased MMP-9 activity and reduced oxidative stress in hypertensive patients, thus suggesting a mechanism probably involved in the pleotropic actions of lercanidipine [16].
  • The cell growth inhibition induced by lercanidipine and its enantiomers was reversible [17].

Anatomical context of Lercanidipine


Associations of Lercanidipine with other chemical compounds


Gene context of Lercanidipine

  • In addition, lercanidipine inhibited the release of metalloproteinases in the extracellular medium (50% and 95% inhibition at 10(-5) M for MMP-9 and MMP-2, respectively) [19].
  • In addition, lercanidipine decreased activated MMP-9 in hypertensive patients without and with diabetes (95% CI, -19 to -47%, P = 0.047, and -80 to -96%, P = 0.010, respectively) [16].
  • A simple, sensitive and rapid ultra-performance liquid chromatography/positive electrospray ionization tandem mass spectrometry (UPLC/ESI-MS/MS) method has been developed and validated for the determination of lercanidipine in human plasma [14].
  • We examined whether lercanidipine produces antioxidant effects and reduces MMP-9 activity in hypertensive patients in a placebo-controlled, crossover, single-blinded design study including 18 healthy volunteers (control group), and 14 hypertensive patients without (N = 7) or with (N = 7) diabetes mellitus [16].
  • To directly rule out the role of calcium channels in the antiatherosclerotic properties of lercanidipine, we examined the effect of the compounds on serum-stimulated calcium influx in SMC [17].

Analytical, diagnostic and therapeutic context of Lercanidipine


  1. Losartan and lercanidipine attenuate low-density lipoprotein oxidation in patients with hypertension and type 2 diabetes mellitus: a randomized, prospective crossover study. Rachmani, R., Levi, Z., Zadok, B.S., Ravid, M. Clin. Pharmacol. Ther. (2002) [Pubmed]
  2. Lercanidipine: a review of its use in hypertension. McClellan, K.J., Jarvis, B. Drugs (2000) [Pubmed]
  3. Effect of lercanidipine and its (R)-enantiomer on atherosclerotic lesions induced in hypercholesterolemic rabbits. Soma, M.R., Natali, M., Donetti, E., Baetta, R., Farina, P., Leonardi, A., Comparato, C., Barberi, L., Catapano, A.L. Br. J. Pharmacol. (1998) [Pubmed]
  4. Calcium antagonists in hypertension: from hemodynamics to outcomes. Messerli, F.H. Am. J. Hypertens. (2002) [Pubmed]
  5. Efficacy and safety of lercanidipine versus hydrochlorothiazide as add-on to enalapril in diabetic populations with uncontrolled hypertension. Agrawal, R., Marx, A., Haller, H. J. Hypertens. (2006) [Pubmed]
  6. Lercanidipine : a review of its efficacy in the management of hypertension. Bang, L.M., Chapman, T.M., Goa, K.L. Drugs (2003) [Pubmed]
  7. Quantification of leg oedema in postmenopausal hypertensive patients treated with lercanidipine or amlodipine. Lund-Johansen, P., Stranden, E., Helberg, S., Wessel-Aas, T., Risberg, K., Rønnevik, P.K., Istad, H., Madsbu, S. J. Hypertens. (2003) [Pubmed]
  8. Antihypertensive efficacy of lercanidipine at 2.5, 5 and 10 mg in mild to moderate essential hypertensives assessed by clinic and ambulatory blood pressure measurements. Multicenter Study Investigators. Omboni, S., Zanchetti, A. J. Hypertens. (1998) [Pubmed]
  9. Role of Ca2+ channels on the hypothermic response produced by activation of kappa-opioid receptors. Gullapalli, S., Nemmani, K.V., Ramarao, P. Pharmacol. Biochem. Behav. (2002) [Pubmed]
  10. Lercanidipine in type II diabetic patients with mild to moderate arterial hypertension. Viviani, G.L. J. Cardiovasc. Pharmacol. (2002) [Pubmed]
  11. Improved tolerability of the dihydropyridine calcium-channel antagonist lercanidipine: the lercanidipine challenge trial. Borghi, C., Prandin, M.G., Dormi, A., Ambrosioni, E. Blood pressure. Supplement. (2003) [Pubmed]
  12. Comparative effects of lercanidipine, lacidipine, and nifedipine gastrointestinal therapeutic system on blood pressure and heart rate in elderly hypertensive patients: the ELderly and LErcanidipine (ELLE) study. Cherubini, A., Fabris, F., Ferrari, E., Cucinotta, D., Antonelli Incalzi, R., Senin, U. Archives of gerontology and geriatrics. (2003) [Pubmed]
  13. Therapeutic profile of manidipine and lercanidipine in hypertensive patients. Casiglia, E., Mazza, A., Tikhonoff, V., Basso, G., Martini, B., Scarpa, R., Pessina, A.C. Advances in therapy. (2004) [Pubmed]
  14. Ultra-performance liquid chromatography/tandem mass spectrometry method for the determination of lercanidipine in human plasma. Kalovidouris, M., Michalea, S., Robola, N., Koutsopoulou, M., Panderi, I. Rapid Commun. Mass Spectrom. (2006) [Pubmed]
  15. Increased vascular selectivity and prolonged pharmacological efficacy of the L-type Ca2+ channel antagonist lercanidipine in human cardiovascular tissue. Brixius, K., Gross, T., Tossios, P., Geissler, H.J., Mehlhorn, U., Schwinger, R.H., Hekmat, K. Clin. Exp. Pharmacol. Physiol. (2005) [Pubmed]
  16. Lercanidipine reduces matrix metalloproteinase-9 activity in patients with hypertension. Martinez, M.L., Lopes, L.F., Coelho, E.B., Nobre, F., Rocha, J.B., Gerlach, R.F., Tanus-Santos, J.E. J. Cardiovasc. Pharmacol. (2006) [Pubmed]
  17. Effect of the new calcium antagonist lercanidipine and its enantiomers on the migration and proliferation of arterial myocytes. Corsini, A., Bonfatti, M., Quarato, P., Accomazzo, M.R., Raiteri, M., Sartani, A., Testa, R., Nicosia, S., Paoletti, R., Fumagalli, R. J. Cardiovasc. Pharmacol. (1996) [Pubmed]
  18. Nephroprotective effect of treatment with calcium channel blockers in spontaneously hypertensive rats. Sabbatini, M., Vitaioli, L., Baldoni, E., Amenta, F. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  19. In vitro inhibitory effect of lercanidipine on cholesterol accumulation and matrix metalloproteinases secretion by macrophages. Canavesi, M., Baldini, N., Leonardi, A., Sironi, G., Bellosta, S., Bernini, F. J. Cardiovasc. Pharmacol. (2004) [Pubmed]
  20. Oxygen-free radical decrease in hypertensive patients treated with lercanidipine. Incandela, L., Belcaro, G., Cesarone, M.R., De Sanctis, M.T., Griffin, M., Cacchio, M., Nicolaides, A.N., Bucci, M., Barsotti, A., Martines, G., Cornelli, U., Di Renzo, A. International angiology : a journal of the International Union of Angiology. (2001) [Pubmed]
  21. L-type Ca2+ channel modulation by dihydropyridines potentiates kappa-opioid receptor agonist induced acute analgesia and inhibits development of tolerance in rats. Gullapalli, S., Ramarao, P. Neuropharmacology (2002) [Pubmed]
  22. Lercanidipine vs lacidipine in isolated systolic hypertension. Millar-Craig, M., Shaffu, B., Greenough, A., Mitchell, L., McDonald, C. Journal of human hypertension. (2003) [Pubmed]
  23. A randomised, double-blind, double-dummy comparison of the efficacy and tolerability of lercanidipine tablets and losartan tablets in patients with mild to moderate essential hypertension. James, I.G., Jones, A., Davies, P. Journal of human hypertension. (2002) [Pubmed]
  24. A selective HPLC method for determination of lercanidipine in tablets. Alvarez-Lueje, A., Pujol, S., Squella, J.A., Núñez-Vergara, L.J. Journal of pharmaceutical and biomedical analysis. (2003) [Pubmed]
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