Fate of 3H- and 14C-labelled A-4166 in pancreatic islets.
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.
Malaisse-Lagae
F
F
Laboratory of Experimental Medicine, Brussels Free University, Erasmus Medical School, Belgium.
Malaisse
W J
WJ
D000818:Animals; D001345:Autoradiography; D002250:Carbon Radioisotopes; D002478:Cells, Cultured; D003510:Cyclohexanes / Q000032:analysis / Q000378:metabolism*; D005260:Female; D007004:Hypoglycemic Agents / Q000032:analysis / Q000378:metabolism*; D007515:Islets of Langerhans / Q000166:cytology / Q000378:metabolism* / Q000648:ultrastructure; D000077715:Nateglinide; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000032:analysis / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D014316:Tritium
D002250:Carbon Radioisotopes; D003510:Cyclohexanes; D007004:Hypoglycemic Agents; D014316:Tritium; D000077715:Nateglinide; D010649:Phenylalanine