Insulinotropic action of meglitinide analogues: modulation by an activator of ATP-sensitive K+ channels and high extracellular K+ concentrations.

  title={Insulinotropic action of meglitinide analogues: modulation by an activator of ATP-sensitive K+ channels and high extracellular K+ concentrations.},
  author={Willy J Malaisse},
  journal={Pharmacological research},
  volume={32 3},
  • W. Malaisse
  • Published 1995
  • Biology, Medicine
  • Pharmacological research
At normal extracellular K+ concentration (5 mM), the meglitinide analogues A-4166, KAD-1229, repaglinide and S3075, all tested at a 10 mu M concentration, markedly enhanced insulin release evoked by 6 mM D-glucose in isolated rat pancreatic islets. They failed, however, to augment the much higher rate of insulin release evoked by D-glucose in islets exposed to a high K+ concentration (30 mM). Under the latter conditions, the potent diazoxide analogue BPDZ-44 (50 mu M) did not exert any sizeable… Expand
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Iglitinide was a less efficient secretagogue than the other non-sulfonylurea hypoglycemic agents and augmented insulin release evoked by either 7 mM D-glucose or 10 microM succinic acid monomethyl ester (SAM). Expand
Combined effects of a calcium-agonist and hypoglycemic or hyperglycemic sulfonamides upon insulin release.
The organic calcium-agonist CGP 28392 augmented insulin release evoked by D-glucose in rat pancreatic islets incubated in the presence or absence of gliclazide, but failed to stimulate insulinExpand
Insulinotropic effect and possible mode of action of a new potent sulfonylurea (BS-4231).
It is suggested that BS-4231 might accelerate within the beta-cell some step of glucose metabolism, which is rate-limiting when the insulin secretory process is not fully stimulated by extracellular glucose. Expand
A pyridothiadiazine (BPDZ 44) as a new and potent activator of ATP-sensitive K+ channels.
The data suggest that BPDZ 44 inhibits the insulin releasing process by activating ATP-sensitive K+ channels, which will lead to a decrease in Ca2+ influx and reduction in [Ca2+]i. Expand
Stimulation of insulin release by non-sulfonylurea hypoglycemic agents: the meglitinide family.
  • W. Malaisse
  • Chemistry, Medicine
  • Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme
  • 1995
Several new non-sulfonylurea hypoglycemic agents such as A-4166, KAD-1229 and repaglinide are structurally related to meglitinide, which exert little effect upon insulin release in nutrient-deprived islets, but markedly augment glucose-stimulated insulin release. Expand
Insulinotropic action of (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl) propionate. I. Secretory and cationic aspects.
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Ionophoretic activity of meglitinide analogues.
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Methods in diabetes research
Partial table of contents: Islet B-Cell Function in Human Subjects (W. Ward et al.) Assessment of Insulin Kinetics in Vivo (J. Radziuk and T. Morishima) Glucose Kinetics: Tracer Methods (E.Expand