PMID: 8955863Nov 1, 1996Paper

Stereo-selective calcium antagonistic and binding properties of the enantiomers of lemildipine in vascular tissue of pigs and dogs

Arzneimittel-Forschung
K NakayamaY Tanaka

Abstract

Stereo-selective calcium antagonistic properties of the enantiomers of lemildipine (CAS 94739-29-4, NB-818) were assessed in vascular tissues, including pig coronary artery and dog cerebral artery. Ca2+ antagonistic action of (-)-lemildipine was about 5 times and 100 times more potent than nifedipine and (+)-lemildipine, respectively. (-), (+), and (+/-)-lemildipine showed a slow onset and long duration of Ca2+ antagonistic action. Pretreatment with (-)-lemildipine and (+/-)-lemildipine for 30 min inhibited the contractions produced by 5-hydroxytryptamine and endothelin-1 with pD2 values between 6.0-8.5, whereas (+)-lemildipine and nifedipine were less potent. Of the lemildipine enantiomers, (+)-lemildipine at a low concentration (1 nmol/l) had a slight but significant Ca2+ agonistic action. However, (+)-lemildipine had no apparent effect on the pCa-tension relationship in the dog basilar artery permeabilized with Staphylococcus aureus alpha-toxin. Enantiomers of lemildipine as well as nifedipine competitively antagonized the specific binding of (+)-[3H]PN 200-110 (isradipine) to the membranes of pig coronary artery in the following order: (-)-lemildipine > nifedipine > (+/-)-lemildipine > (+)-lemildipine. These results suggest...Continue Reading

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