Selective antagonists at group I metabotropic glutamate receptors: synthesis and molecular pharmacology of 4-aryl-3-isoxazolol amino acids
Research output: Contribution to journal › Journal article › Research › peer-review
Homologation of (S)-glutamic acid (Glu, 1) and Glu analogues has previously provided ligands with activity at metabotropic Glu receptors (mGluRs). The homologue of ibotenic acid (7), 2-amino-3-(3-hydroxy-5-isoxazolyl)propionic acid (HIBO, 8), and the 4-phenyl derivative of 8, compound 9a, are both antagonists at group I mGluRs. Here we report the synthesis and molecular pharmacology of HIBO analogues 9b-h containing different 4-aryl substituents. All of these compounds possess antagonist activity at group I mGluRs but are inactive at group II and III mGluRs.
Original language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 45 |
Issue number | 4 |
Pages (from-to) | 988-91 |
ISSN | 0022-2623 |
Publication status | Published - 14 Feb 2002 |
- Animals, Brain, CHO Cells, Cricetinae, Cyclic AMP, Electrophysiology, Excitatory Amino Acid Antagonists, Hydrolysis, Isoxazoles, Phosphatidylinositols, Radioligand Assay, Rats, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Research areas
ID: 45613794