FURTHER CHARACTERICATION OF AGONIST EFFECTS OF FLUMAZENIL

氟马西尼激动剂作用的进一步表征

• 批准号: 6277212
• 负责人: Warren K Bickel
• 金额: $ 2.62万
• 依托单位: UNIVERSITY OF VERMONT & ST AGRIC COLLEGE
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-12-01 至 1998-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6277212
• 关键词: benzodiazepine receptor; benzodiazepines; caffeine; drug interactions; human subject; inhibitor /antagonist; midazolam; sensory discrimination

This study is a continuation of our assessment of the discriminative stimulus effects of flumazenil, a benzodiazepine receptor antagonist. That study demonstrated that flumazenil (0.56 mg/70 kg) is readily discriminated from saline. In addition, substitution tests with various doses of flumazenil (0, 0.10, 0.32 and 1.0 mg/70 kg) demonstrated dose- dependent increases on several self-report measures sensitive to sedative- like effects (e.g., PCAG subscale of the ARCI, sedative rating on the adjective rating scale) in the 6 subjects who completed the study. This study is being conducted in order to determine whether the observed agonist effects of flumazenil are benzodiazepine-like by training a flumazenil (0.56 mg/70 kg) versus saline discrimination and then conducting substitution tests with three test doses of midazolam (1.0, 1.8, and 3.2 mg/70 kg). The substitution tests are being conducted under a novel-response drug discrimination procedure, which offers subjects a response alternative appropriate for effects unlike flumazenil or saline. Self-reported effects of flumazenil and midazolam are also being compared. In addition, we are testing one dose of caffeine (75 mg/70 kg) as a negative control. Three subjects have completed this study. Thus far, results indicate that flumazenil and midazolam have similar, but not identical, discriminative stimulus effects in humans.

本研究是我们对歧视性评估的延续