Antagonism of benzodiazepine binding in rat and human brain by antiliriumR
| Autor: | Kermit V Speeg, Steven Schenker, M. Lawrence Berman, Sherry Wang, G. R. Avant |
|---|---|
| Rok vydání: | 1979 |
| Předmět: |
Physostigmine
Time Factors medicine.drug_class In Vitro Techniques Pharmacology General Biochemistry Genetics and Molecular Biology Flurazepam Non-competitive inhibition medicine Animals Humans General Pharmacology Toxicology and Pharmaceutics Receptor Benzodiazepine Diazepam Chemistry Brain General Medicine Human brain Rats Kinetics medicine.anatomical_structure Anti-Anxiety Agents Depression Chemical Cholinergic Flunitrazepam medicine.drug |
| Zdroj: | Life Sciences. 24:1345-1350 |
| ISSN: | 0024-3205 |
| DOI: | 10.1016/0024-3205(79)90003-1 |
| Popis: | Physostigmine (Antilirium R ) has been reported to reverse benzodiazepine- induced sleep or coma in man and prevent death in animals. Accordingly, we investigated the effect of Antilirium upon benzodiazepine binding to both rat and human brain. We report that Antilirium inhibits 3 H-diazepam and 3 H-flunitrazepam binding in a dose-dependent manner. The degree of inhibition of binding by Antilirium correlates with the affinity of benzodiazepine for its “receptor” such that diazepam is more affected than flunitrazepam. The inhibition is rapid but the kinetics are complex with only doses of Antilirium showing competitive inhibition when studied at equilibrium. These results may explain, at least in part, the effectiveness of Antilirium at reversing benzodiazepine-induced hypnosis without necessarily implicating a cholinergic mechanism. |
| Databáze: | OpenAIRE |
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