An Orally Bioavailable, Functionally Selective Inverse Agonist at the Benzodiazepine Site of GABAA α5 Receptors with Cognition Enhancing Properties
| Autor: | W. Rycroft, George R. Marshall, Neil Collinson, Mark Stuart Chambers, Angus Murray Macleod, Gerard R. Dawson, John R. Atack, Susan M. Cook, Desmond O'Connor, Sarah Christine Hobbs, Pushpindar Ferris, Robert W. Carling |
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| Rok vydání: | 2004 |
| Předmět: |
Patch-Clamp Techniques
medicine.drug_class Administration Oral Biological Availability Pharmacology Mice Radioligand Assay Cognition Dogs Oral administration Drug Discovery medicine Animals Inverse agonist GABA-A Receptor Agonists Maze Learning Receptor Nootropic Agents Benzodiazepine Binding Sites Triazines GABAA receptor Chemistry Biological activity Isoxazoles Receptors GABA-A Rats Protein Subunits Anxiogenic Convulsant Molecular Medicine |
| Zdroj: | Journal of Medicinal Chemistry. 47:5829-5832 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | (3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (13) has been identified as a functionally selective, inverse agonist at the benzodiazepine site of GABA(A) alpha5 receptors. 13 is orally bioavailable, readily penetrates the CNS, and enhances performance in animal models of cognition. It does not exhibit the convulsant, proconvulsant, or anxiogenic activity associated with nonselective GABA(A) inverse agonists. |
| Databáze: | OpenAIRE |
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