Doenicke A, Suttmann H, Kapp W, Kugler J, Ebentheuer H
Anaesthesist. 1984 Aug;33(8):343-7.
The benzodiazepine-receptors are close by the GABA-receptors. They are found in all areas of the brain, especially in the area of the cortex. The imidazo-benzodiazepine Ro 15-1788 has a high affinity to the receptor without showing any biological activity. The antagonist Ro 15-1788 cancels the sleeping effect, which was produced by benzodiazepines, within 30-60 s. Deep phases of sleep after 4 mg per 70 kg body weight lormetazepam, a dose which was not in clinical use up to now as well as the sleeping effect of 2 mg flunitrazepam per 70 kg body weight and 10-11 mg midazolam per 70 kg body weight are safely antagonized without adverse reactions. According to pharmacodynamic researches by means of EEG and psychometry the half-life period of the antagonist is shorter (1-2 h) than that of the agonist. The clinical application of the antagonist Ro 15-1788 (in patients) is at hand. The control of benzodiazepine-N2O/O2-anaesthesia seems to be guaranteed with the introduction of the antagonist for clinical use.
苯二氮䓬受体靠近γ-氨基丁酸（GABA）受体。它们存在于大脑的所有区域，尤其是皮质区域。咪唑并苯二氮䓬Ro 15 - 1788对该受体具有高亲和力，但不显示任何生物活性。拮抗剂Ro 15 - 1788可在30 - 60秒内消除苯二氮䓬类药物产生的睡眠效果。每70千克体重服用4毫克氯美扎酮（该剂量目前尚未用于临床）后的深睡眠阶段，以及每70千克体重服用2毫克氟硝西泮和每70千克体重服用10 - 11毫克咪达唑仑后的睡眠效果，均可被安全拮抗且无不良反应。根据通过脑电图和心理测量学进行的药效学研究，拮抗剂的半衰期（1 - 2小时）比激动剂的半衰期短。拮抗剂Ro 15 - 1788（在患者中）的临床应用即将实现。随着拮抗剂用于临床，苯二氮䓬-氧化亚氮/氧气麻醉的控制似乎有了保障。
