互动pinaverium(季铵化合物),在大鼠回肠平滑肌4-dihydropyridine结合位点。

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Feron O, Wibo M, Christen莫,Godfraind T

互动pinaverium(季铵化合物),在大鼠回肠平滑肌4-dihydropyridine结合位点。

Br J杂志。1992年2月,105 (2):480 - 4。

PubMed ID

1313732 (在PubMed

]

文摘

1。pinaverium溴的交互,季铵化合物,结合位点(l型钙通道阻滞剂)研究在大鼠回肠平滑肌。2。Pinaverium抑制[3 h] - (+) pn200 - 110 ([3 h] - (+) -isradipine)特定的绑定组织匀浆不完全(Ki 0.38 microM;最大抑制80%)。相比之下,绑定到单个细胞制剂(通过胶原酶治疗)和saponin-treated匀浆完全被抑制。这些数据是兼容的观点,在未经处理的匀浆,20%的[3 h] - (+) -isradipine pinaverium绑定网站无法访问,因为它与密封由内向外囊泡相关联。3所示。Pinaverium溴化增加了明显的KD [3 h] - (+) -isradipine绑定saponin-treated匀浆,但没有明显影响Bmax值。此外,离解速率常数[3 h] - (+) -isradipine绑定被pinaverium没有改变。 These data suggest that pinaverium interacts with the dihydropyridine binding site in a competitive manner. However, in contrast to uncharged dihydropyridine calcium antagonists, pinaverium inhibited, rather than stimulated, [3H]-diltiazem binding to rat brain membranes (at 30-37 degrees C). 4. Although Bmax values of [3H]-(+)-isradipine were similar in homogenates prepared from tissue and cells (collagenase-treated), the KD value was significantly higher in cell homogenates (166 vs 95 pM). Similarly, the Ki value of pinaverium was higher in cell preparations than in tissue homogenates (0.77 vs 0.38 microM). Thus, collagenase can significantly modify the dihydropyridine recognition site.5. The competitive interaction of pinaverium, a permanently charged drug, with [3H]-(+)-isradipine bound to intact cells and its absence of interaction with [3H]-(+)-isradipine bound to sealed inside-out vesicles imply that the dihydropyridine receptor lies near the external surface of the plasma membrane.

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药物

Pinaverium

药物靶点

药物	目标	类	生物	药理作用	行动
Pinaverium	压敏电阻器l型钙通道亚基alpha -	蛋白质	人类	是的	拮抗剂 抑制剂	细节