THE DESIGN AND SYNTHESES OF PHOTOAFFINITY PROBES FOR L-GLUTAMIC ACID NEURORECEPTORS (INDANE).

摘要

Eighty-five chemicals were tested for L-glutamic acid neuroreceptor binding in a synaptosomal assay. Based on these results, two photoaffinity probes, gamma-L-glutamyl-para-azidoanilide and gamma-N-L-glutamyl-6-azido-2-naphthylamide, were synthesized. Another synthetic product, gamma-N-L-glutamyl-6-nitro-2-naphthylamide, showed promise as a fluorescent affinity probe.; Several indane derivatives were also synthesized. Two of these, 1-amino-1-carboxy-2,2-dimethyl-3-indanone and spiro-(2,2-dimethyl-3-indanone)-1,5'- hydantoin, displayed anticonvulsive activity when tested in mice challenged with the convulsive agent pentylenetetrazol. In addition, these compounds provide a pathway to other interesting chemicals, including 1,3-diamino-1,3-dicarboxy-2,2-dimethyl-indane, spiro-(2,2-dimethyl-indane)-1,5'-3,5'-dihydantoin, and photosensitive azido derivatives of these compounds.