| 摘要 |
Compounds of a class of alkyl carboxy amino acid analogs of glutamic acid according to formula I act as specific regulators of kainic acid EAA receptor cation channel, wherein R<1> is 1) CH3, or 2) halogen; R<2> and R<3> are independently 1) H, 2) C1-C6-alkyl, 3) C3-C4-alkenyl, 4) C3-C5-cycloalkyl, 5) C1-C6-alkyl-CO-, 6) C1-C6-alkyl-OCO-, 7) C1-C6-alkyl-NHCO-, 8) CHO-, or 9) C3-C6-alkynyl; R<2> and R<3> taken together can be -CH2(CH2)pCH2-; p is 0, 1, 2 or 3; and pharmaceutically acceptable salts of these compounds, but not including compounds of Formula I wherein R<2> and R<3> are H and R<1> is CH3 or R<1> is F. These compounds are useful for treating neurological, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacological and functional disorders associated with excessive or insufficient activation of the kainic acid subtype of the ionotropic EAA receptors; treating cognitive disorders associated with deactivation, suboptimal activation or over-activation of the kainic acid receptor; alleviating pain and improving and enhancing memory, learning, and associated mental processes. A method for designing novel AMPA or kainic acid receptor agonists or antagonists is also disclosed. |
