Fate of 3H- And 14C-labelled A-4166 in Pancreatic Islets

Acta Diabetol. 1996 Dec;33(4):298-300. doi: 10.1007/BF00571569.


The fate of 3H- and 14C-labelled A-4166 was examined in rat pancreatic islets. The net uptake of the meglitinide analogue by islets incubated for 60 min in the presence of 0.1 mM A-4166 and then submitted to repeated washes was close to 0.1 pmol/islet. It was significantly increased when the concentration of D-glucose in the incubation medium was raised from 2.8 to 16.7 mM. No sizeable internalization of tritiated A-4166 into insulin-producing cells could be detected by autoradiography. These findings suggest that the interaction of A-4166 with the beta-cell may be restricted to its insertion on the plasma membrane and binding to sulphonylurea receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Autoradiography
  • Carbon Radioisotopes
  • Cells, Cultured
  • Cyclohexanes / analysis
  • Cyclohexanes / metabolism*
  • Female
  • Hypoglycemic Agents / analysis
  • Hypoglycemic Agents / metabolism*
  • Islets of Langerhans / cytology
  • Islets of Langerhans / metabolism*
  • Islets of Langerhans / ultrastructure
  • Nateglinide
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / analysis
  • Phenylalanine / metabolism
  • Rats
  • Rats, Wistar
  • Tritium


  • Carbon Radioisotopes
  • Cyclohexanes
  • Hypoglycemic Agents
  • Tritium
  • Nateglinide
  • Phenylalanine