Reves J G, Corssen G, Holcomb C
Can Anaesth Soc J. 1978 May;25(3):211-4. doi: 10.1007/BF03004881.
Ro 21-3981 is a newly synthesized water soluble benzodiazepine derivative. Its pharmacological properties are similar to diazepam. This investigation was designed to establish the effective induction dosage of Ro 21-3981 and to compare it with diazepam for induction of anaesthesia. The ED50 for Ro 21-3981 induction is 0.15 mg/kg and ED 100 is 0.2 mg/kg. Ro 21-3981 is one and one-half times as potent as diazepam (0.3 mg/kg) and more rapid in action. There is significantly less pain on injection with Ro 21-3981 as compared to diazepam. Cardiovascular stability and apnoea were observed with both drugs. Ro 21-3981 is a promising anaesthetic induction drug that merits further human study.
Ro 21-3981是一种新合成的水溶性苯二氮䓬衍生物。其药理特性与地西泮相似。本研究旨在确定Ro 21-3981的有效诱导剂量，并将其与地西泮用于麻醉诱导进行比较。Ro 21-3981诱导的半数有效剂量（ED50）为0.15毫克/千克，完全有效剂量（ED100）为0.2毫克/千克。Ro 21-3981的效力是地西泮（0.3毫克/千克）的1.5倍，且起效更快。与地西泮相比，注射Ro 21-3981时的疼痛明显减轻。两种药物均观察到心血管稳定性和呼吸暂停。Ro 21-3981是一种有前景的麻醉诱导药物，值得进一步开展人体研究。
