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Bioorg. Med. Chem. Lett. · May 2004
Effect of gabapentin derivates on mechanical allodynia-like behaviour in a rat model of chronic sciatic constriction injury.
- Yang Hong-Ju, Liu He, Shi Wei-Guo, Zhao Nan, Yuan Wei-Xiu, Jiang Zhong-Wei, Wang Jun-Wei, Gong Zheng-Hua, Zhong Bo-Hua, Luo Zhi-Pu, and Gong Zhe-Hui.
- Beijing Institute of Pharmacology and Toxicology, Pharmacology Department, Taiping Road 27, Beijing 100850, China. yanghongju618@sina.com
- Bioorg. Med. Chem. Lett. 2004 May 17;14(10):2537-41.
AbstractA series of mutual prodrugs derived 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.
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