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Open AccessArticle

Synthesis and Analgesic Activity Evaluation of Some Agmatine Derivatives

1
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, 110016, P.R. China
2
Department of Medicinal Chemistry, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P.R. China
*
Author to whom correspondence should be addressed.
Molecules 2006, 11(6), 393-402; https://doi.org/10.3390/11060393
Received: 10 May 2006 / Accepted: 9 June 2006 / Published: 12 June 2006
A series of N,N’-disubstituted-2-nitroethene-1,1-diamine and N,N’-disubstituted- N’’-cyanoguanidine derivatives were prepared and evaluated for in vivo analgesic activity. The blood brain barrier (BBB) VolSurf model was used to predict the BBB permeation profiles of our synthesized compounds. Some compounds show both remarkable analgesic activity and good BBB permeation profiles, and these compounds might be developed for treatment of opioid tolerance and dependence. View Full-Text
Keywords: Agmatine derivatives; synthesis; analgesic activity; blood-brain barrier; opioid dependence. Agmatine derivatives; synthesis; analgesic activity; blood-brain barrier; opioid dependence.
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He, H.; Liu, M.; Zheng, Z.; Liu, Y.; Xiao, J.; Su, R.; Hu, C.; Li, J.; Li, S. Synthesis and Analgesic Activity Evaluation of Some Agmatine Derivatives. Molecules 2006, 11, 393-402.

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