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РЖ ВИНИТИ 34 (BI48) 97.09-04Т2.48

Stereo-selective calcium antagonistic and binding properties of the enantiomers of lemildipine in vascular tissue of pigs and dogs [Text] / Koichi Nakayama [et al.] // Arzneim.-Forsch. - 1996. - Vol. 46, N 11. - P1045-1053 . - ISSN 0004-4172
Перевод заглавия: Стереоселективность свойств энантиомеров лемилдипина как антагонистов кальция, а также их связывания в тканях сосудов свиней и собак
Аннотация: 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. Ca{2+} 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 Ca{2+} antagonistic action. Pretreatment with (-)-lemildipine and ('+-')-lemildipine for 30 min inhibited the contractions produced by 5-hydroxytryptamine and endothelin-1 with pD[2] 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 Ca{2+} agonistic action. However, (+)-lemildipine had no apparent effect on the pCa-tension relationship in the dog basilar artery permeabilized with Staphylococcus aureus 'альфа'-toxin. Enantiomers of lemildipine as well as nifedipine competitively antagonized the specific binding of (+)-[{3}H]PN 200-110 (isradipine) to the membranes of pig coronary artery in the following order: (-)-lemildipinenifedipine('+-')-lemildipine(+)-lemildipine. These results suggest that the stereo-selective Ca{2+} antagonistic actions of lemildipine enantiomers and nifedipine assessed in the functional experiments were well correlated with their potencies for the competition with the (+)-[{3}H]PN 200-110 binding to the pig coronary artery. Библ. 38

ГРНТИ	34.45.21

ВИНИТИ 341.45.21.29.15.09.19 + 341.45.21.83.09
Рубрики: ЛЕМИЛДИПИН
ЭНАНТИОМЕРЫ
СТЕРЕОСЕЛЕКТИВНОСТЬ
АНТАГОНИСТЫ КАЛЬЦИЯ
КОРОНАРНЫЕ АРТЕРИИ
АРТЕРИИ МОЗГА
СВИНЬИ
СОБАКИ

Доп.точки доступа:
Nakayama, Koichi; Nakazawa, Tohru; Fukuta, Yoshihisa; Tanaka, Yoshio

РЖ ВИНИТИ 34 (BI05) 97.10-04И8.78

Stereo-selective calcium antagonistic and binding properties of the enantiomers of lemildipine in vascular tissue of pigs and dogs [Text] / Koichi Nakayama [et al.] // Arzneim.-Forsch. - 1996. - Vol. 46, N 11. - P1045-1053 . - ISSN 0004-4172
Перевод заглавия: Стереоселективность свойств энантиомеров лемилдипина как антагонистов кальция, а также их связывания в тканях сосудов свиней и собак
Аннотация: 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. Ca{2+} 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 Ca{2+} antagonistic action. Pretreatment with (-)-lemildipine and ('+-')-lemildipine for 30 min inhibited the contractions produced by 5-hydroxytryptamine and endothelin-1 with pD[2] 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 Ca{2+} agonistic action. However, (+)-lemildipine had no apparent effect on the pCa-tension relationship in the dog basilar artery permeabilized with Staphylococcus aureus 'альфа'-toxin. Enantiomers of lemildipine as well as nifedipine competitively antagonized the specific binding of (+)-[{3}H]PN 200-110 (isradipine) to the membranes of pig coronary artery in the following order: (-)-lemildipinenifedipine('+-')-lemildipine(+)-lemildipine. These results suggest that the stereo-selective Ca{2+} antagonistic actions of lemildipine enantiomers and nifedipine assessed in the functional experiments were well correlated with their potencies for the competition with the (+)-[{3}H]PN 200-110 binding to the pig coronary artery. Библ. 38

ГРНТИ	34.39.57

ВИНИТИ 341.39.57.09
Рубрики: ЛЕМИЛДИПИН
ЭНАНТИОМЕРЫ
СТЕРЕОСЕЛЕКТИВНОСТЬ
АНТАГОНИСТЫ КАЛЬЦИЯ
КОРОНАРНЫЕ АРТЕРИИ
АРТЕРИИ МОЗГА
СВИНЬИ
СОБАКИ

Доп.точки доступа:
Nakayama, Koichi; Nakazawa, Tohru; Fukuta, Yoshihisa; Tanaka, Yoshio

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