The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain
| Autor: | Derek N. Middlemiss, Tania O. Stean, Neil Upton, Jeff Jerman, Hugh J. Herdon, Wai Chan |
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| Rok vydání: | 1996 |
| Předmět: |
Pharmacology
medicine.medical_specialty Binding Sites Membranes Seizure threshold Stereochemistry Chemistry medicine.medical_treatment Biological activity Mice Membrane Endocrinology Anticonvulsant Stereospecificity Prosencephalon Mechanism of action Internal medicine Forebrain Benzamides medicine Animals Anticonvulsants Benzopyrans Binding site medicine.symptom |
| Zdroj: | European journal of pharmacology. 314(3) |
| ISSN: | 0014-2999 |
| Popis: | The novel compound SB 204269 ( trans -(+)-6-acetyl-4 S -(4-fluorobenzoylamino)-3,4-dihydro-2,2-dimethyl-2 H -benzo[ b ]pyran-3 R -ol,hemihydrate) shows potent anticonvulsant activity in the mouse maximal electroshock seizure threshold test. The binding of [ 3 H]SB 204269 to mouse forebrain membranes is saturable ( B max 217 fmol/mg protein, K d 32 nM) and stereospecific. The excellent anticonvulsant profile of SB 204269, combined with the identification of a unique central binding site for the compound, suggest that it has potential clinical utility as a novel treatment for epilepsy. |
| Databáze: | OpenAIRE |
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