Molecular mechanisms of vasoselectivity of the 1,4-dihydropyridine lercanidipine

British Journal of Pharmacology

Volumn 142, Issue 2, 2004, Pages 275-284

  Wirtz, Susanne ^a   Herzig, Stefan ^a  

^a UNIVERSITY OF COLOGNE   (Germany)

Author keywords

Ca v1.2; Dihydropyridine; Lercanidipine; Vasoselectivity

Indexed keywords

1,4 DIHYDROPYRIDINE DERIVATIVE; CALCIUM CHANNEL L TYPE; CALCIUM CHANNEL STIMULATING AGENT; LERCANIDIPINE;

ACIDITY; ANIMAL CELL; ARTICLE; BLOOD VESSEL FUNCTION; CHO CELL; CONTROLLED STUDY; DEPOLARIZATION; DRUG EFFECT; DRUG MECHANISM; DRUG POTENCY; ENANTIOSELECTIVITY; FEMALE; IC 50; MOLECULAR DYNAMICS; NONHUMAN; PATCH CLAMP; PH; PRIORITY JOURNAL; STANDARDIZATION; STEREOCHEMISTRY;

ANIMALS; CALCIUM CHANNELS, L-TYPE; CHO CELLS; CRICETINAE; DIHYDROPYRIDINES; DOSE-RESPONSE RELATIONSHIP, DRUG; ENDOTHELIUM, VASCULAR; PROTEIN ISOFORMS; RABBITS;

EID: 2942514366     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0705786     Document Type: Article

References (34)

1. ANGELICO, P., GUARNERI, A., LEONARDI, A. & TESTA, R. (1999). Vascular-selective effect of lercanidipine and other 1,4-dihydropyridines in isolated rabbit tissues. J. Pharm. Pharmacol., 51, 709-714.
2. BAINDUR, N., RUTLEDGE, A. & TRIGGLE, D.J. (1993). A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels. J. Med. Chem., 36, 3743-3745.
3. BANGALORE, R., BAINDUR, N., RUTLEDGE, A., TRIGGLE, D.J. & KASS, R.S. (1994). L-type calcium channels: asymmetrical intramembrane binding domain revealed by variable length, permanently charged 1,4-dihydropyridines. Mol. Pharmacol., 46, 660-666.
4. BEAN, B.P. (1984). Nitrendipine block of cardiac calcium channels: high affinity binding to the inactivated state. Proc. Natl. Acad. Sci. U.S.A., 81, 6388-6392.
5. BECHEM, M. & HOFFMANN, H. (1993). The molecular mode of action of the Ca agonist (-) Bay K 8644 on the cardiac Ca channel. Pflügers Arch., 424, 343-353.
6. BOSSE, E., BOTTLENDER, R., KLEPPISCH, T., HESCHELER, J., WELLING, A., HOFMANN, F. & FLOCKERZI, V. (1992). Stable and functional expression of the calcium channel α1 subunit from smooth muscle in somatic cell lines. EMBO J., 11, 2033-2038.
7. CERBAI, E., BARBIERI, M. & MUGELLI, A. (1997). Electrophysiologic study of lercanidipine and its enantiomers. J. Cardiovasc. Pharmacol., 29 (Suppl. 1), S1-S9.
8. GUARNERI, L., ANGELICO, P., IBBA, M., POGGESI, E., TADDEI, C., LEONARDI, A. & TESTA, R. (1996). Pharmacological in vitro studies of the new 1,4-dihydropyridine calcium antagonist lercanidipine. Arzneimittelforschung, 46, 15-24.
9. GUARNERI, L., SIRONI, G., ANGELICO, P., IBBA, M., GRETO, L., COLOMBO, D., LEONARDI, A. & TESTA, R. (1997). In vitro and in vivo vascular selectivity of lercanidipine and its enantiomers. J. Cardiovasc. Pharmacol., 29 (Suppl. 1), S25-S32.
10. 2+ channel block by dihydropyridines: no modulation by the voltage protocol. Eur. J. Pharmacol., 309, 317-321.
11. 2+ channels by two different mechanisms. J. Physiol (London), 521.1, 31-42.
12. HEATH, B., XIA, J. & KASS, R.S. (1997). Molecular pharmacology of UK-118, 434-05, a permanently charged amlodipine analog. Int. J. Cardiol., 62 (Suppl. 2), S47-S54.
13. HESS, P., LANSMAN, J.B. & TSIEN, R.W. (1984). Different modes of Ca channel gating behaviour favoured by dihydropyridine Ca agonists and antagonists. Nature, 311, 538-544.
14. HUGHES, A.D. & WIJETUNGE, S. (1993). The action of amlodipine on voltage-operated calcium channels in vascular smooth muscle. Br. J. Pharmacol., 109, 120-125.
15. 0 on calcium channel block by amlodipine, a charged dihydropyridine compound. J. Gen. Physiol., 93, 1109-1127.
16. KASS, R.S., ARENA, J.P. & DIMANNO, D. (1988). Block of heart calcium channels by amlodipine: influence of drug charge on blocking activity. J. Cardiovasc. Pharmacol., 12 (Suppl. 7), S45-S49.
17. KAWASHIMA, Y. & OCHI, R. (1988). Voltage-dependent decrease in the availability of single calcium channels by nitrendipine in guinea-pig ventricular cells. J. Physiol. (London), 402, 219-235.
18. KOKUBUN, S., PROD'HOM, B., BECKER, C., PORZIG, H. & REUTER, H. (1986). Studies on Ca channels in intact cardiac cells: voltage-dependent effects and cooperative interactions of dihydropyridine enantiomers. Mol. Pharmacol., 30, 571-584.
19. LACERDA, A.E. & BROWN, A.M. (1989). Nonmodal gating of cardiac calcium channels as revealed by dihydropyridines. J. Gen. Physiol., 93, 1243-1273.
20. LACINOVA, L., AN, H.R., XIA, J., ITO, H., KLUGBAUER, N., TRIGGLE, D., HOFMANN, F. & KASS, R.S. (1999). Distinctions in the molecular determinants of charged and neutral dihydropyridine block of L-type calcium channels. J. Pharmacol. Exp. Ther., 289, 1472-1479.
21. 2+ channels. NaunynSchmiedeberg's Arch. Pharmacol., 360, 122-128.
22. LEONARDI, A., POGGESI, E., TADDEI, C., GUARNERI, L., ANGELICO, P., ACCOMAZZO, M.R., NICOSIA, S. & TESTA, R. (1997). In vitro calcium antagonist activity of lercanidipine and its enantiomers. J. Cardiovasc. Pharmacol., 29 (Suppl. 1), S10-S18.
23. 1-subunits. Br. J. Pharmacol., 125, 1005-1012.
24. PERI, R., PADMANABHAN, S., RUTLEDGE, A., SINGH, S. & TRIGGLE, D.J. (2000). Permanently charged chiral 1,4-dihydropyridines: molecular probes of L-type calcium channels. Synthesis and pharmacological characterization of methyl (ω-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3- nitrophenyl)-3,5-pyridine-dicarboxylate iodide, calcium channel antagonists. J. Med. Chem., 43, 2906-2914.
25. PETERSON, B.Z. & CATTERALL, W.A. (1995). Calcium binding in the pore of L-type calcium channels modulates high affinity dihydropyridine binding. J. Biol. Chem., 270, 18201-18204.
26. 2+ currents in atrial myocytes. Pflügers Arch., 420, 410-412.
27. SANGUINETTI, M.C. & KASS, R.S. (1984). Voltage-dependent block of calcium channel current in the calf cardiac Purkinje fiber by dihydropyridine calcium channel antagonists. Circ. Res., 55, 336-348.
28. SCHRÖDER, F., HANDROCK, R., BEUCKELMANN, D.J., HIRT, S., HULLIN, R., PRIEBE, L., SCHWINGER, R.H.G., WEIL, J. & HERZIG, S. (1998). Increased availability and open probability of single L-type calcium channels from failing compared with non-failing human ventricle. Circulation, 98, 969-976.
29. SIRONI, G., COLOMBO, D., GRETO, L., TESTA, R. & LEONARDI, A. (1997). Antihypertensive activity of lercanidipine and its enantiomers in animal models. J, Cardiovasc. Pharmacol., 29 (Suppl. 1), S33-S40.
30. STRAUER, B.E. (1974). Inotropic effects of nifedipine: a new coronary dilating agent. Int. J. Clin. Pharmacol., 9, 101-107.
31. THOMAS, G., GROSS, R. & SCHRAMM, M. (1984). Calcium channel modulation: ability to inhibit or promote calcium influx resides in the same dihydropyridine molecule. J. Cardiovasc. Pharmacol., 6, 1170-1176.
32. WELLING, A., KWAN, Y.W., BOSSE, E., FLOCKERZI, V., HOFMANN, F. & KASS, R.S. (1993). Subunit-dependent modulation of recombinant L-type calcium channels: molecular basis for dihydropyridine tissue selectivity. Circ. Res., 73, 974-980.
33. 2+ channels. Circ. Res., 81, 526-532.
34. WIRTZ, S. & HERZIG, S. (2003). Molecular mechanisms of the vasoselectivity of a new dihydropyridine, (S)-lercanidipine. Naunyn-Schmiedeberg's Arch. Pharmacol., 367, R65 (248).