The inhibitory effects of YZG-330/YZG-331 on central nervous system
10.3969/j.issn.1001-1978.2018.06.010
- VernacularTitle:腺苷衍生物差向异构体YZG-330和YZG-331的中枢抑制作用比较研究
- Author:
Wan-Qi YANG
1
;
Shao-Bo JIA
;
Xu-Lin LI
;
Yu ZHANG
;
Xiao-Wei ZHOU
;
Zheng-Gang YUE
;
Cheng-Gen ZHU
;
Jian-Gong SHI
;
Jian-Jun ZHANG
Author Information
1. 中国医学科学院北京协和医学院药物研究所药理室
- Keywords:
central nervous system;
locomotor activity;
epimeride;
LORR;
glutamic acid;
γ-aminobutyric acid
- From:
Chinese Pharmacological Bulletin
2018;34(6):785-789
- CountryChina
- Language:Chinese
-
Abstract:
Aim To investigate the inhibitory effects of the novel compounds YZG-330 and YZG-331 in central nervous system. Methods The sedative effect was investigated by recording the spontaneous locomotor ac-tivity in mice. The hypnotic effect was evaluated by the latency and duration of the loss of righting reflex ( LORR) in the threshold dosage of sodium pentobarbi-tal treated mice. The two compounds induced the mice that had woken up after a threshold dosage pentobarbi-tal sodium to fall asleep again. The levels of GABA and Glu in brain were measured by HPLC-ECD. Re-sults The results showed that spontaneous locomotor activities decreased in YZG-330 (0.125, 0.5,2 mg·kg-1 ) treated mice and YZG-331 (1.25, 5, 20 mg· kg-1 ) treated mice. YZGs could extend the duration of the loss of righting reflex in threshold dosage of sodium pentobarbital treated mice, and significantly shorten sleep latency. YZGs were able to allow the mice that had woken up after a threshold dosage pentobarbital so-dium to fall asleep again. YZG-331 (40 mg·kg-1 ,i. g. ) could significantly increase GABA level in hypo-thalamus and cerebral cortex. The content of GABA had no significant change after YZG-330 ( 2 mg · kg-1 , ig. ) administration. Conclusions YZG-330 and YZG-331 have potent sedative and hypnotic effects. The efficacy of YZG-330 is stronger than that of YZG-331 , but the mechanism of two compounds sounds different.
