PHARMACODYNAMIC/PHARMACOKINETICS STUDY OF ZALEPLON AND ZOLPIDEM

扎来普隆和唑吡坦的药效学/药代动力学研究

• 批准号: 6275689
• 负责人: DAVID J GREENBLATT
• 金额: $ 4.05万
• 依托单位: TUFTS MEDICAL CENTER
• 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/6275689
• 关键词: blood chemistry; clinical research; clinical trials; drug screening /evaluation; electroencephalography; human subject; neuropharmacology; pharmacokinetics; psychopharmacology; pyrazolopyrimidine; sedative /hypnotic

Zalepon (CL-284846) is a novel, pyrazolopyrimidine, sedative-hypnotic which binds weakly but differentially to the GABA Brian complex. In animal models, it produced potent sedative and anticonvulsive effects similar to marketed benzodiazepines. In tests for side effect potential, zalepon, unlike most marketed sedatives, produced no hangover effect, exhibited less propensity for memory loss, reduced tolerance, (suggesting a lower potential for abuse), and at an efficacious dose showed a reduced tendency to pontentiate depressant effects with alcohol. In addition, human pharmacokinetic data predict a fast onset and elimination (t max and t1/2 are approximately 1 hour). Based on the medical need for improved sedative-hypnotics and the results of preclinical and clinical studies thus far insomnia with fewer side effects than are commonly associated with most drugs currently marketed for this purpose.

Zalepon（CL-284846）是一种新型吡唑并嘧啶类镇静催眠药 其与GABA布莱恩复合物的结合较弱但有差异。 在 动物模型，它产生了强大的镇静和抗惊厥作用 类似于市售的苯二氮卓。在潜在副作用测试中， 与大多数市售镇静剂不同，扎来朋不产生宿醉效果， 表现出较少的记忆丧失倾向，耐受性降低，（表明 滥用的可能性较低），并且在有效剂量下， 倾向于推测酒精的副作用。此外，本发明还提供了一种方法， 人体药代动力学数据预测快速起效和消除（Tmax和 t1/2约为1小时）。 基于医疗需求的改善 镇静催眠药及临床前和临床研究结果 到目前为止，失眠症的副作用比通常的失眠症少。 目前市场上的大多数药物都是用于此目的。