In vitro mechanism of action on insulin release of S-22068, a new putative antidiabetic compound.

ABSTRACT: 1. The MIN6 cell line derived from in vivo immortalized insulin-secreting pancreatic beta cells was used to study the insulin-releasing capacity and the cellular mode of action of S-22068, a newly synthesized imidazoline compound known for its antidiabetic effect in vivo. 2. S-22068, was able to release insulin from MIN6 cells in a dose-dependent manner with a half-maximal stimulation at 100 micronM. Its efficacy (8 fold over the basal value), which did not differ whatever the glucose concentration (stimulatory or not), was intermediate between that of sulphonylurea and that of efaroxan. 3. Similarly to sulphonylureas and classical imidazolines, S-22068 blocked K(ATP) channels and, in turn, opened nifedipine-sensitive voltage-dependent Ca2+ channels, triggering Ca2+ entry. 4. Similarly to

SUBMITTER: Le Brigand L 

PROVIDER: S-EPMC1571726 | biostudies-literature | 1999 Nov

REPOSITORIES: biostudies-literature