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Canavanine induces insulin release via activation of imidazoline I 3 receptors
Author(s) -
Yang TingTing,
Niu HoShan,
Chen LiJen,
Ku PoMing,
Lin KaoChang,
Cheng JueiTang
Publication year - 2015
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/1440-1681.12348
Subject(s) - imidazoline receptor , canavanine , agmatine , receptor , chinese hamster ovary cell , endocrinology , chemistry , insulin , medicine , agonist , pharmacology , biology , biochemistry , arginine , amino acid
Summary The aim of the present study was to identify the effect of canavanine on the imidazoline receptor because canavanine is a guanidinium derivative that has a similar structure to imidazoline receptor ligands. Transfected Chinese hamster ovary‐K1 cells expressing imidazoline receptors (nischarin ( NISCH )‐ CHO ‐K1 cells) were used to elucidate the direct effects of canavanine on imidazoline receptors. In addition, the imidazoline I 3 receptor has been implicated in stimulation of insulin secretion from pancreatic β ‐cells. Wistar rats were used to investigate the effects of canavanine (0.1, 1 and 2.5 mg/kg, i.v.) on insulin secretion. In addition the a specific I 3 receptor antagonist KU 14R (4 or 8 mg/kg, i.v.) was used to block I 3 receptors. Canavanine decreased blood glucose by increasing plasma insulin in rats. In addition, canavanine increased calcium influx into NISCH ‐ CHO ‐K1 cells in a manner similar to agmatine, the endogenous ligand of imidazoline receptors. Moreover, KU 12R dose‐dependently attenuated canavanine‐induced insulin secretion in HIT ‐T15 pancreatic β ‐cells and in the plasma of rats. The data suggest that canavanine is an agonist of I 3 receptors both in vivo and in vitro . Thus, canavanine would be a useful tool in imidazoline receptor research.