Effects of the novel dihydropyridine derivative niguldipine on the cytoplasmic free calcium concentration of mouse thymocytes.
Niguldipine, a novel dihydropyridine derivative, was tested for its effects on the cytoplasmic free Ca2+ concentration of mouse thymocytes. In quin-2-loaded cells, a concentration-dependent rise of cytoplasmic Ca2+ can be detected, which requires extracellular Ca2+. The effect of niguldipine reaches a maximum after about 5 min; a similar time course has been observed, when using concanavalin A as a stimulus. Niguldipine provokes influx of Ca2+ into thymocytes, but not of Mn2+. Moreover, the effect of niguldipine exhibits some degree of stereospecificity, since (-)-niguldipine was more effective than its (+)-enantiomer. The action of niguldipine could be reversed by addition of bovine serum albumin, but not by addition of nitrendipine. None of several agents tested (e.g. felodipine, nitrendipine, trifluoperazine, cloxacepride, phenylephrine and ouabain) could mimic the effect of niguldipine at a concentration of 1 microM.
Drozd
M P
MP
Department of Pharmacology and Toxicology, University of Ulm, Ulm/Donau, Federal Republic of Germany.
Gietzen
K
K
D000818:Animals; D002118:Calcium / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D002478:Cells, Cultured; D004095:Dihydropyridines / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D008297:Male; D051379:Mice; D012709:Serum Albumin / Q000494:pharmacology; D013237:Stereoisomerism; D013950:Thymus Gland / Q000187:drug effects* / Q000378:metabolism
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D012709:Serum Albumin; D002118:Calcium; C054074:niguldipine