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- Title
Canavanine induces insulin release via activation of imidazoline I<sub>3</sub> receptors.
- Authors
Yang, Ting‐Ting; Niu, Ho‐Shan; Chen, Li‐Jen; Ku, Po‐Ming; Lin, Kao‐Chang; Cheng, Juei‐Tang
- Abstract
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 I3 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 I3 receptor antagonist KU14R (4 or 8 mg/kg, i.v.) was used to block I3 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, KU12R 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 I3 receptors both in vivo and in vitro. Thus, canavanine would be a useful tool in imidazoline receptor research.
- Subjects
CANAVANINE; INSULIN; IMIDAZOLINES; GUANIDINE; LABORATORY rats
- Publication
Clinical & Experimental Pharmacology & Physiology, 2015, Vol 42, Issue 3, p263
- ISSN
0305-1870
- Publication type
Article
- DOI
10.1111/1440-1681.12348