McNicholas L F, Martin W R
Drug Alcohol Depend. 1986 Jul;17(4):339-48. doi: 10.1016/0376-8716(86)90083-9.
CGS-8216, a benzodiazepine antagonist, was administered to rats acutely dosed with diazepam, and to rats chronically dosed with diazepam or pentobarbital. The effects of an acute dose of diazepam were antagonized by CGS-8216 but signs of precipitated abstinence were not observed. An apparent arousing effect was seen in non-dependent rats when CGS-8216 was administered after placebo, but no arousal was observed when Ro15-1788 was administered after placebo in non-dependent rats. A precipitated abstinence syndrome was elicited with CGS-8216 in rats chronically dosed with diazepam and was very similar to the abstinence syndrome precipitated by Ro15-1788 in diazepam-dependent rats. Like Ro15-1788, CGS-8216 elevated Precipitated Abstinence Scale (PAS) scores in a dose-related manner until a plateau was reached with 5 mg/kg. No signs of precipitated abstinence were observed when CGS-8216 was administered to rats dependent on phenobarbital.
苯二氮䓬拮抗剂CGS - 8216被给予急性注射地西泮的大鼠，以及长期注射地西泮或戊巴比妥的大鼠。急性剂量的地西泮的作用被CGS - 8216拮抗，但未观察到戒断反应加剧的迹象。在非依赖性大鼠中，安慰剂后给予CGS - 8216时可见明显的兴奋作用，但在非依赖性大鼠中，安慰剂后给予Ro15 - 1788时未观察到兴奋作用。CGS - 8216在长期注射地西泮的大鼠中引发了戒断综合征，且与Ro15 - 1788在依赖地西泮的大鼠中引发的戒断综合征非常相似。与Ro15 - 1788一样，CGS - 8216以剂量相关的方式提高了戒断反应量表（PAS）评分，直至达到5mg/kg的平台期。当给依赖苯巴比妥的大鼠注射CGS - 8216时，未观察到戒断反应加剧的迹象。
