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

Synthesis and Analgesic Activity Evaluation of Some Agmatine Derivatives

Hongxia He 1 , Mengjia Liu 1 email, Zhibing Zheng 2,* email, Ying Liu 2 email, Junhai Xiao 2 email, Ruibin Su 2 email, Chun Hu 1 email, Jin Li 2 email and Song Li 2 email
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.

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Cite This Article

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.

AMA 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(6):393-402.

Chicago/Turabian Style

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.

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