(2S)-2-苄基-3-(顺式六氢-2-异吲哚啉基羰基)丙酸酯的促胰岛素作用。II. 离子电泳和构象方面
Insulinotropic action of (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl) propionate. II. Ionophoretic and conformational aspects.
作者信息
Malaisse W J, Nadi A B, Malaisse-Lagae F, Sato F, Lins L, Brasseur R
机构信息
Laboratoires de Médecine Expérimentale et de Chimie Physique des Macromolécules aux Interfaces, Brussels Free University, Belgium.
出版信息
Gen Pharmacol. 1995 Oct;26(6):1319-25. doi: 10.1016/0306-3623(94)00316-f.
PMID:7590126
Abstract
- The non-sulphonylurea insulinotropic agent sodium (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl) propionate (KAD-1229) was found to display calcium ionophoretic activity in an artificial membrane model. 2. Conformation analysis indicated that a complex between calcium and KAD-1229, with a 1:2 stoichiometry, indeed displays favourable attributes for ionophoretic activity across a hydrophobic environment. 3. It is speculated that the ionophoretic property of KAD-1229 might participate to the remodelling of cationic fluxes evoked by this insulinotropic agent in pancreatic islet cells.
摘要
- 非磺酰脲类促胰岛素分泌剂（2S）-2-苄基-3-（顺式六氢-2-异吲哚啉基羰基）丙酸钠（KAD-1229）在人工膜模型中显示出钙离子载体活性。2. 构象分析表明，钙与KAD-1229之间形成的化学计量比为1:2的复合物确实具有在疏水环境中进行离子载体活性的有利特性。3. 据推测，KAD-1229的离子载体特性可能参与了该促胰岛素分泌剂在胰岛细胞中引起的阳离子通量重塑。
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