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synthesis and analgesic activity evaluation of some agmatine derivatives合成和镇痛活性评价的胍基丁胺衍生品.pdf

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synthesis and analgesic activity evaluation of some agmatine derivatives合成和镇痛活性评价的胍基丁胺衍生品

Molecules 2006, 11, 393-402 molecules ISSN 1420-3049 Full Paper Synthesis and Analgesic Activity Evaluation of Some Agmatine Derivatives Hongxia He 1, Mengjia Liu 1, Zhibing Zheng 2,*, Ying Liu 2, Junhai Xiao 2, Ruibin Su 2, Chun 1 2 2 Hu , Jin Li and Song Li 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 E-mail addresses: Zhibing ZHENG: zbzheng@, Mengjia Liu: mj32800@, Ying Liu: luxin314@, Junhai Xiao: xiaojunhai@, Ruibin Su: Ruibinsu@Y, Chun HU: Chem2000@163.com, Jin Li: lijin@, Song LI: lis@ *Author to whom correspondence should be addressed; e-mail: hhx110015@ 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. Introduction Agmatine (1, Figure 1) is an endogenous ligand of imidazoline receptors [1], and is biologically active in the nervous system and many other tissues in mammals [2]