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目的:研究硝苯地平、氨氯地平和(+)SM-6586预处理过的大鼠脑膜与[~3H]伊拉地平观察结合密度的变化.方法:用大鼠脑膜,该脑浆膜与硝苯地平(10 nmol L~(-1)),氨氯地平(1μmol L~(-1)),SM-6586(1 nmol L~(-1))以及不加拮抗剂分别预保温45 min,离心,所得沉淀用缓冲液清洗,3次后与[~3H]伊拉地平一起保温,通过Scatchard解析求出用钙拮抗剂预处理后膜成分的K_d和B_(max)值.结果:硝苯地平对[~3H]伊拉地平取代位置的拮抗可以通过清洗而减弱,特殊取代显示出很低的值.但通过氨氯地平和SM-6586拮抗后,在同样条件下拮抗不易被减弱.以上这些药物的K_d值都没有明显的变化.结论:氨氯地平和SM-6586对脑膜中钙通道拮抗的分解过程是缓慢的.
OBJECTIVE: To study the change of binding density of [~ 3H] irabandine pretreated with nifedipine, amlodipine and (+) SM-6586.Methods: Rat brain membrane, (10 nmol L -1), amlodipine (1 μmol L -1), SM-6586 (1 nmol L -1), and no antagonist for 45 min, Centrifuged, and the resulting precipitate was washed with buffer and incubated with [~ 3H] iradipine three times, and the K_d and B max values of the membrane components after calcium pretreatment were determined by Scatchard analysis.Results: Antagonism of the site of [~ 3H] -laplatin substitution can be weakened by washing, and the special substitution shows a very low value, but antagonism by amlodipine and SM-6586 is not easily weakened under the same conditions. There was no significant change in the K_d values of these drugs.Conclusion: Amlodipine and SM-6586 are slow to antagonize the calcium channel in the meninges.