A23187与降血糖磺酰脲类药物的同源和杂化钙络合物：核磁共振与构象分析

Homologous and hybrid calcium complexes of A23187 and hypoglycemic sulfonylureas: nuclear magnetic resonance and conformational analysis.

作者信息

Deleers M, Brasseur R, Gelbcke M, Malaisse W J

出版信息

J Inorg Biochem. 1982 Jun;16(3):215-25. doi: 10.1016/s0162-0134(00)80108-7.

Abstract

Hypoglycemic sulfonylureas (e.g., gliclazide) are able to transport calcium across hydrophobic domains. Gliclazide and the ionophore A23187 act synergistically upon calcium transport. One calcium atom is complexed by either two molecules of sulfonylureas (or A23187) or one molecule each of sulfonylurea and A23187; the existence of such hybrid complexes has been documented by nuclear magnetic resonance. Conformation analysis of the calcium-gliclazide complex suggests close apposition of the toluyl groups in the gliclazide molecules.

摘要

降血糖磺酰脲类药物（如格列齐特）能够跨疏水结构域转运钙。格列齐特与离子载体A23187在钙转运方面具有协同作用。一个钙原子可与两个磺酰脲分子（或A23187）络合，或与一个磺酰脲分子和一个A23187分子各络合一个；这种混合络合物的存在已通过核磁共振得到证实。钙 - 格列齐特络合物的构象分析表明，格列齐特分子中的甲苯基紧密相邻。