Insulinotropic action of (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl) propionate. II. Ionophoretic and conformational aspects.
1. 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.
Malaisse
W J
WJ
Laboratoires de Médecine Expérimentale et de Chimie Physique des Macromolécules aux Interfaces, Brussels Free University, Belgium.
Nadi
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Malaisse-Lagae
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Sato
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Lins
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Brasseur
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D000818:Animals; D002118:Calcium / Q000378:metabolism / Q000494:pharmacology; D002412:Cations / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology*; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D007476:Ionophores; D054833:Isoindoles; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats
D002412:Cations; D007004:Hypoglycemic Agents; D007211:Indoles; D007476:Ionophores; D054833:Isoindoles; C087255:mitiglinide; D002118:Calcium