Modulation of native GABA(A) receptor activity by triazolo 1,5-benzodiazepines
| Autor: | Giancarlo Grossi, Mauro Robello, Aroldo Cupello, Elena Gatta, M Di Braccio, Periklis Nikas, Francesca Pellistri |
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| Rok vydání: | 2013 |
| Předmět: |
Agonist
Benzodiazepine Patch-Clamp Techniques GABAA receptor Chemistry medicine.drug_class General Neuroscience 5-benzodiazepines Biological activity Pharmacology Receptors GABA-A GABA-A receptors GABAA-rho receptor Rats Rats Sprague-Dawley Benzodiazepines 1 Flumazenil Cerebellum medicine Animals Flunitrazepam Receptor medicine.drug |
| Zdroj: | Neuroscience. 243 |
| ISSN: | 1873-7544 |
| Popis: | In previous work our group described the synthesis and the activity on rat cerebellum granule cell GABAA receptors of new 1,5-benzodiazepine compounds. Here we are describing the synthesis of new triazolobenzodiazepines (mainly 1,5-benzodiazepine derivatives) and the evaluation of their biological activity in terms of effects on those GABAA receptors. Their effects were compared to those of 1,4-benzodiazepine agonists and some known 1,5-benzodiazepines. The activities were evaluated for the two GABAA receptor populations present in cerebellar granule cells, one mediating phasic inhibition and the other one mediating tonic inhibition. Some of the compounds displayed a profile of agonist at the component mediating phasic inhibition. This agonistic activity was prevented by the benzodiazepine site antagonist flumazenil. Interestingly, the active compounds displayed an agonistic activity at these receptors significantly greater than that of “classical” 1,4-benzodiazepine agonists, such as diazepam, flunitrazepam and alprazolam. |
| Databáze: | OpenAIRE |
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