Abstract
Ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124, 4) is a member of a new generation of ultra-short acting hypnotics. HIE-124 (4) exhibited potent in vivo activity with a rapid onset of action and a short duration of action, with no acute tolerance or noticeable side effects. The metabolic profile of 4 is also performed. HIE-124 (4) has the potential use as a preanesthetic medication, anesthesia inducer, and could be used with thiopental sodium to maintain anesthesia for longer duration.
MeSH terms
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Animals
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Azepines / metabolism*
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Azepines / pharmacokinetics
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Azepines / pharmacology*
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Carboxylic Acids / metabolism*
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Carboxylic Acids / pharmacokinetics
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Carboxylic Acids / pharmacology*
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Dose-Response Relationship, Drug
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Hypnotics and Sedatives / chemical synthesis
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Hypnotics and Sedatives / metabolism*
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Hypnotics and Sedatives / pharmacokinetics
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Hypnotics and Sedatives / pharmacology*
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Mice
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Thiazoles / metabolism*
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Thiazoles / pharmacokinetics
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Thiazoles / pharmacology*
Substances
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8-oxo-5,6,7,8-tetrahydro-thiazolo(3,2-a)(1,3)diazepin-3-carboxylate
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Azepines
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Carboxylic Acids
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Hypnotics and Sedatives
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Thiazoles