Anti-fatigue activity screening of novel positive allosteric modulators on AMPA receptor
10.3969/j.issn.1001-1978.2018.03.017
- VernacularTitle:新型AMPA受体正向变构调节剂抗疲劳活性筛选
- Author:
Yao CHEN
1
;
Shu-Mei MA
;
Qi-Bing MEI
;
Li LIU
Author Information
1. 中国医药工业研究总院药理评价研究中心
- Keywords:
AMPA receptor;
benzamide;
cytotoxicity;
central excitability;
burden swimming experiment;
an-ti-fatigue
- From:
Chinese Pharmacological Bulletin
2018;34(3):382-387
- CountryChina
- Language:Chinese
-
Abstract:
Aim To explore the novel anti-fatigue a-gents targeting AMPA receptor. Methods Three ben-zoic acids of different methoxy substitutions were em-ployed, including piperonylic acid, 3,4,5-trimethoxy benzoic acid and 3,4-dimethoxy benzoic acid, which as mother nucleus and cyclic aliphatic amine or pheny-lpiperazine derivatives were introduced to modify the nitrogen atoms connecting to amino bonds. Forty-three compounds were synthesized and identified by 1 H-NMR. MTT assay, then pentobarbital induced hypno-sis experiment and mice burden swimming experiment were applied respectively to evaluate the new synthesized compounds’ cytotoxicity, CNS excitability and anti-fatigue activity. Results Compound 2j had low cytotoxicity,presenting certain central excitability and significant advantages on anti-fatigue. Conclusion The further development of compounds 2j with good anti-fatigue activities could be cultivated in further study.
