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Synthesis and Analgesic Activity Evaluation of Some Agmatine Derivatives
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, 110016, P.R. China
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
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.
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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.
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(6):393-402.
He, Hongxia; Liu, Mengjia; Zheng, Zhibing; Liu, Ying; Xiao, Junhai; Su, Ruibin; Hu, Chun; Li, Jin; Li, Song. 2006. "Synthesis and Analgesic Activity Evaluation of Some Agmatine Derivatives." Molecules 11, no. 6: 393-402.