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Molecules 2006, 11(6), 393-402; doi:10.3390/11060393

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.
Received: 10 May 2006 / Accepted: 9 June 2006 / Published: 12 June 2006
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Abstract

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.
Keywords: Agmatine derivatives; synthesis; analgesic activity; blood-brain barrier; opioid dependence. Agmatine derivatives; synthesis; analgesic activity; blood-brain barrier; opioid dependence.
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

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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