Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amines / administration & dosage
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Amines / chemical synthesis*
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Amines / pharmacology*
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Animals
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Chronic Disease
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Cyclohexanecarboxylic Acids / administration & dosage
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Cyclohexanecarboxylic Acids / chemical synthesis*
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Cyclohexanecarboxylic Acids / pharmacology*
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Cyclohexanols / administration & dosage
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Cyclohexanols / chemical synthesis
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Cyclohexanols / pharmacology
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Disease Models, Animal
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Gabapentin
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Memantine / administration & dosage
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Memantine / chemical synthesis
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Memantine / pharmacology
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Pain / drug therapy
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Pain Threshold / drug effects
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Pregabalin
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Prodrugs / chemical synthesis
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Rats
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Sciatic Neuropathy / drug therapy*
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Structure-Activity Relationship
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Venlafaxine Hydrochloride
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gamma-Aminobutyric Acid / administration & dosage
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gamma-Aminobutyric Acid / analogs & derivatives*
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gamma-Aminobutyric Acid / chemical synthesis*
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gamma-Aminobutyric Acid / pharmacology*
Substances
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Amines
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Cyclohexanecarboxylic Acids
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Cyclohexanols
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Prodrugs
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Pregabalin
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gamma-Aminobutyric Acid
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Gabapentin
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Venlafaxine Hydrochloride
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Memantine