Effect of gabapentin derivates on mechanical allodynia-like behaviour in a rat model of chronic sciatic constriction injury

A series of mutual prodrugs were synthesized and their pharmacological properties to treat allodynia were investigated. A series of mutual prodrugs derivated from gabapentin, pregabalin, memantine, venlafaxine were synthesized and their pharmacological properties to treat neuropathic pain were inves...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-05, Vol.14 (10), p.2537-2541
Hauptverfasser: Hong-Ju, Yang, He, Liu, Wei-Guo, Shi, Nan, Zhao, Wei-Xiu, Yuan, Zhong-Wei, Jiang, Jun-Wei, Wang, Zheng-Hua, Gong, Bo-Hua, Zhong, Zhi-Pu, Luo, Zhe-Hui, Gong
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Sprache:eng
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Zusammenfassung:A series of mutual prodrugs were synthesized and their pharmacological properties to treat allodynia were investigated. A series of mutual prodrugs derivated from gabapentin, pregabalin, memantine, venlafaxine were synthesized and their pharmacological properties to treat neuropathic pain were investigated in a rat model of chronic sciatic nerve constriction injury (CCI). In vivo evaluation demonstrated that the mutual prodrugs 2002413A, 2002823A composed of two gabapentins, 2002414 composed of gabapentin and pregabalin were effective in reversal tactile allodynia in CCI rats. The prodrugs 2002413A, 2002414 had no significant influence on the rotarod activity. The result suggest that the prodrugs may be possible candidates for further development.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.02.094