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首页> 外文期刊>Research communications in molecular pathology and pharmacology >Binding of tritiated S21403 to an artificial phospholipid bilayer.
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Binding of tritiated S21403 to an artificial phospholipid bilayer.

机译：ti化的S21403与人工磷脂双层的结合。

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摘要

The binding of tritiated S21403, a novel insulin-releasing agent of the meglitinide family, to multilamellar liposomes formed of egg yolk phosphatidylcholine was compared to that of tritiated glibenclamide. The binding of [3H]S21403 reached equilibrium within 5 min of incubation at 37 degrees C, was virtually proportional to its concentration (2.8 to 56.0 nM) and failed to be inhibited by a much higher concentration (0.1 mM) of unlabelled S21403. It was much lower than that of [3H]glibenclamide tested at a comparable concentration (14.8 nM) and only slightly decreased by 0.1 mM unlabelled glibenclamide. The latter sulfonylurea inhibited more severely the binding of [3H]glibenclamide, which was unaffected, however, by 0.1 mM unlabelled S21403. These findings suggest a much higher affinity of glibenclamide than S21403 for the artificial phospholipid bilayer, this coinciding with a higher biological potency, as insulin secretagogue, of the hypoglycemic sulfonylurea as compared to meglitinide analog. It is proposed, therefore, that the insertion of these antidiabetic agents in the phospholipid domain of the B-cell membrane may condition their access to the ATP-responsive K+ channels known to represent the main target for their insulinotropic action.
机译：将ti化的S21403（一种美格替尼家族的新型胰岛素释放剂）与蛋黄磷脂酰胆碱形成的多层脂质体的结合与tri化的格列本脲的结合进行了比较。 [3H] S21403的结合在37°C下孵育5分钟内达到平衡，实际上与其浓度（2.8至56.0 nM）成正比，并且未受到更高浓度（0.1 mM）的未标记S21403的抑制。它远低于在相当浓度（14.8 nM）下测试的[3H]格列本脲的含量，并且仅略微降低了0.1 mM的未标记格列本脲。后者的磺酰脲可更严重地抑制[3H] glibenclamide的结合，但是该结合不受0.1 mM未标记的S21403的影响。这些发现表明，与S21403相比，格列本脲对人工磷脂双层具有更高的亲和力，这与降血糖的磺酰脲相比，与美格列奈类似物具有更高的生物学效力，如胰岛素促分泌剂。因此，建议将这些抗糖尿病药插入B细胞膜的磷脂结构域可能会限制其进入已知代表其促胰岛素作用主要靶点的ATP反应性K +通道。

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