AI Article Synopsis
- YZG-331 is a synthetic derivative of NHBA with strong sedative and hypnotic effects, and the research aims to understand its mechanism of action.
- YZG-331 reduces spontaneous movement in mice, and this effect is blocked by adenosine receptor antagonists, suggesting it works through specific receptors.
- The study also found that YZG-331 decreases intracellular calcium levels and CaMKII phosphorylation, indicating that it influences calcium signaling pathways to produce its sedative effects.
Article Abstract
YZG-331 is a synthetic novel derivates of N-(4-hydroxybenzyl) adenine riboside (NHBA), which has potent sedative and hypnotic effects based on our previous study. We are now aiming to investigate the mechanism of YZG-331. In this research, the behavioral studies showed that YZG-331 (4, 8, 16 mg/kg, i.g.) could reduce the spontaneous locomotor activity in mice, which could be blocked by AM (non-selective adenosine receptor antagonist), DPCPX (adenosine A receptor (AR) antagonist), and SCH58261 (adenosine A receptor (AR) antagonist). Moreover, YZG-331 no longer exerted sedative effect in AR or AR knockdown mice. YZG-331 (2.5, 5, 10 mg/kg, i.g.) prolonged sleeping time in pentobarbital sodium treated mice, which can be prevented by DPCPX or SCH58261. The above results demonstrated that YZG-331 exerted sedative and hypnotic effects through AR and AR. In addition, it was found that YZG-331 (25, 50, 100 μM) decreased intracellular calcium level and YZG-331 (10 mg/kg, i.g.) decreased CaMKII phosphorylation (pCaMKII) level in mouse hypothalamus and cortex. In summary, this study indicated that activation of AR/ AR and down regulation of Ca-CaMKII signaling pathway were involved in the sedative and hypnotic effects of YZG-331.
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| http://dx.doi.org/10.1016/j.bbr.2022.113885 | DOI Listing |
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