Insulinotropic action of (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl) propionate. II. Ionophoretic and conformational aspects.

Malaisse, W. J.; Nadi, A. B.; Malaisse-Lagae, F.; Sato, F.; Lins, Laurence; Brasseur, Robert

doi:10.1016/0306-3623(94)00316-F

Article (Scientific journals)

Insulinotropic action of (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl) propionate. II. Ionophoretic and conformational aspects.

Malaisse, W. J.; Nadi, A. B.; Malaisse-Lagae, F. et al.

1995 • In General Pharmacology, 26 (6), p. 1319-25

Peer Reviewed verified by ORBi

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https://hdl.handle.net/2268/63800

DOI
10.1016/0306-3623(94)00316-F

PubMed
7590126

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Keywords :

Animals; Calcium/metabolism/pharmacology; Cations/metabolism; Hypoglycemic Agents/chemistry/pharmacology; Indoles/chemistry/pharmacology; Ionophores; Isoindoles; Models, Molecular; Molecular Structure; Rats

Abstract :

[en] 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.

Disciplines :

Biochemistry, biophysics & molecular biology

Author, co-author :

Malaisse, W. J.

Nadi, A. B.

Malaisse-Lagae, F.

Sato, F.

Lins, Laurence ; Université de Liège - ULiège > Gembloux Agro-Bio Tech

Brasseur, Robert ; Université de Liège - ULiège > Gembloux Agro-Bio Tech

Language :

English

Title :

Insulinotropic action of (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl) propionate. II. Ionophoretic and conformational aspects.

Publication date :

1995

Journal title :

General Pharmacology

ISSN :

0306-3623

Publisher :

Elsevier Science, Exeter, United Kingdom

Volume :

Issue :

Pages :

1319-25

Peer reviewed :

Peer Reviewed verified by ORBi

Available on ORBi :

since 25 June 2010

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Bibliography

Brasseur, Ruysschaert (1986) Conformation and mode of organization of amphiphilic membrane components: a conformational analysis. Biochem. J. 238:1-11.
Brasseur (1991) Differentiation of lipid associating helices by use of tridimensional molecular hydrophobicity potential calculation. J. Biol. Chem. 266:16,120-16,127.
Couturier, Malaisse (1980) Ionophoretic activity of hypoglycemic sulfonylureas. Arch. Int. Pharmacodyn. 245:323-334.
Couturier, Malaisse (1986) Insulinotropic effects of hypoglycaemic and hyperglycaemic sulfonamides the ionophoretic hypothesis. Diabetologia 19:335-340.
Deleers, Brasseur (1989) Physico-chemical properties of prostaglandins and related pharmacological compounds: a theoretical study on conformational related activity. Biochem. Pharmacol. 38:2441-2447.
Deleers, Grognet, Mahy, Brasseur, Malaisse (1983) Synergistic effect of hypoglycemic sulfonyl-ureas and negative phospholipids on calcium transport: ionic and conformational aspects. Res. Commun. Chem. Pathol. Pharmacol. 41:407-424.
Hopfinger Conformational Properties of Macromolecules, Academic Press, New York; 1973.
Malaisse, Sato (1995) Insulinotropic action of (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarboxyl) propionate. I. Secretory and cationic aspects in rat pancreatic islets. Gen. Pharmac. 26:1313-1318.
Malaisse, Hubinont, Lebrun, Herchuelz, Couturier, Deleers, Malaisse-Lagae, Sener (1983) Mode of action of hypoglycaemic sulfonylureas in the pancreatic β-cells: coinciding and conflicting views. Clinical and Pharmacological Activities of Sulfonylurea Drugs , M. Serrano-Rios, L.P. Krahl, Excerpta Medica, Amsterdam; 24-38.
Nelder, Mead (1965) A simplex method for function minimization. The Computer Journal 7:308-313.
Ohnota, Koizumi, Tsutumi, Kobayashi, Inoue, Sato (1994) Novel rapid- and short-acting hypoglycemic agent, a calcium (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionate (KAD-1229) that acts on the sulfonylurea receptor: comparison of effects between KAD-1229 and gliclazide. J. Pharmacol. Exp. Ther. 269:489-495.
Tanford The Hydrophobic Effect: Formation of Micelles and Biological Membranes, Wiley, New York; 1973.