| Autor: |
Kozikowski AP; Drug Discovery Program, Georgetown University Medical Center, Washington, DC 20007-2197, USA., Steensma D, Varasi M, Pshenichkin S, Surina E, Wroblewski JT |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 1998 Mar 03; Vol. 8 (5), pp. 447-52. |
| DOI: |
10.1016/s0960-894x(98)00052-3 |
| Abstrakt: |
Syntheses of both the alpha-methyl and benzyl analogs of quisqualic acid are described. Testing of these compounds for their activity at excitatory amino acid receptors revealed a striking change in activity in comparison to quisqualic acid. This structural modification results in the loss of quisqualate's potent agonist action at both non-NMDA ionotropic glutamate receptors as well as at group I mGluRs, while allowing these analogs to acquire antagonist properties with relative selectivity for group II metabotropic glutamate receptors. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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