Abstract：
:Novel insulinotropic agent nateglinide stimulates insulin via binding to sulfonylurea receptor and closing the ATP-dependent K+ (K(ATP)) channels in pancreatic beta-cells, leading to an increase in [Ca(2+)](i) for exocytosis. The voltage-dependent Ca(2+) channel and the delayed rectifier K+ (Kv) channels are also present in beta-cells and their activities determine the configuration of action potential and hence contribute to the regulation of [Ca(2+)](i) and insulin secretion. This study, by using the patch-clamp method in whole cell configuration, comparatively characterized the direct effects of sulfonylurea receptor ligands including nateglinide, glyburide, and repaglinide on Kv and Ca(2+) channels. Each agent inhibited Kv currents in a concentration-dependent manner with effective concentration range two to three orders higher than that for blocking K(ATP) channels. A marginal stimulation of Ca(2+) current was observed with all drugs, while repaglinide at concentration greater than 300 nM inhibited Ca(2+) current. The direct effects of these antidiabetic agents on Kv and Ca(2+) channels may act concertedly with their primary action on K(ATP) channels in regulating [Ca(2+)](i) and the stimulus-secretion coupling.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Hu S,Wang Sdoi
10.1016/s0014-2999(01)01252-3keywords:
subject
Has Abstractpub_date
2001-09-14 00:00:00pages
97-104issue
2eissn
0014-2999issn
1879-0712pii
S0014-2999(01)01252-3journal_volume
427pub_type
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