@article{APS7019,
author = {Ying-li QU and Chiyo TAKAMIZAWA and Kentaro SUGIYMA and Keiko MARUYAMA and Kaoru HATTORI and Kenichi WATANABE and Takafumi NAGATOMO},
title = {Residual inhibition in density of [3H]isradipine binding sites in rat brain membrane pretreated with amlodipine},
journal = {Acta Pharmacologica Sinica},
volume = {16},
number = {4},
year = {2016},
keywords = {},
abstract = {AIM: To test changes in the density of [3H] isradipine binding sites in rat brain membrane pretreated with amlodipine and to compare with those of nifedipine and (+) SM-6586 (methyl 1, 4-dihydro-2, 6-dimethyl-3-(3-(N-benzyl-N-methylaminomethyl)-1,2,4- oxadiazolyl-5-yl)-4-(3-nitrophenyl) pyridine-5-carboxylate).
METHODS: The membrane-enriched fractions were prepared from rat brain. The brain membranes were preincubated with nifedipine (10 nmol L-1), amlodipine (1 mumol L-1) and SM-6586 (1 nmol L-1) or with no antagonists added for 45 min, and washing and centrifugation were performed 3 times. They were assayed with [3H]isradipine in incubation media. The Kd and Bmax values of the membrane fractions pretreated with the drugs were determined by Scatchard analysis.
RESULTS: The blockage of the [3H]isradipine binding sites induced by nifedipine was reversed by washing, enabling the low values of the specific binding sites to be observed. The blockages by amlodipine and SM-6586, on the other hand, were not readily reversed. No significant difference was found, however, between in the Kd walues of these drugs.
CONCLUSION: Amlodipine and SM-6586 are Ca2+ antagonists which dissociate slowly from the Ca2+ channel in membranes.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/7019}
}