Abstract
The synthesis, unambiguous proof of structure and benzodiazepine receptor affinity and efficacy of 2-phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one 1 are reported. The in vitro biological data indicate that 1 may be the lead compound of a new class of benzodiazepine antagonist-inverse agonist ligands.
MeSH terms
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Animals
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Benzoxazines
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Binding, Competitive / drug effects
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Brain / drug effects
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Brain / metabolism
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Cattle
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Crystallography, X-Ray
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Flunitrazepam / pharmacokinetics
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In Vitro Techniques
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Ligands
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Magnetic Resonance Spectroscopy
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Oxazines / chemical synthesis*
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Oxazines / pharmacology
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Receptors, GABA-A / drug effects*
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Triazoles / chemical synthesis*
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Triazoles / pharmacology
Substances
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Benzoxazines
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Ligands
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Oxazines
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Receptors, GABA-A
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Triazoles
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2-phenyl-1,2,4-triazolo(1,5-c)(1,3)benzoxazin-5-one
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Flunitrazepam