Document Detail

Effect of gabapentin derivates on mechanical allodynia-like behaviour in a rat model of chronic sciatic constriction injury.
MedLine Citation:
PMID:  15109646     Owner:  NLM     Status:  MEDLINE    
A 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.
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; Gong Zhe-Hui
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  14     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2004 May 
Date Detail:
Created Date:  2004-04-27     Completed Date:  2004-12-22     Revised Date:  2013-08-21    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  2537-41     Citation Subset:  IM    
Beijing Institute of Pharmacology and Toxicology, Pharmacology Department, Taiping Road 27, Beijing 100850, China.
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MeSH Terms
Amines / administration & dosage,  chemical synthesis*,  pharmacology*
Chronic Disease
Cyclohexanecarboxylic Acids / administration & dosage,  chemical synthesis*,  pharmacology*
Cyclohexanols / administration & dosage,  chemical synthesis,  pharmacology
Disease Models, Animal
Memantine / administration & dosage,  chemical synthesis,  pharmacology
Pain / drug therapy
Pain Threshold / drug effects
Prodrugs / chemical synthesis
Sciatic Neuropathy / drug therapy*
Structure-Activity Relationship
gamma-Aminobutyric Acid / administration & dosage,  analogs & derivatives*,  chemical synthesis*,  pharmacology*
Reg. No./Substance:
0/Amines; 0/Cyclohexanecarboxylic Acids; 0/Cyclohexanols; 0/Prodrugs; 19982-08-2/Memantine; 55JG375S6M/pregabalin; 56-12-2/gamma-Aminobutyric Acid; 6CW7F3G59X/gabapentin; GRZ5RCB1QG/venlafaxine

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