Sanger D J
Laboratoires d'Etudes et de Recherches Synthélabo (L.E.R.S.), Bagneux, France.
Psychopharmacology (Berl). 1987;93(3):365-8. doi: 10.1007/BF00187258.
The effects of Ro 16-6028 and Ro 17-1812, two novel benzodiazepines with mixed agonist and antagonist properties, were studied in rats trained to discriminate either chlordiazepoxide or the benzodiazepine receptor ligand zolpidem. In rats discriminating 5 mg/kg chlordiazepoxide from saline both Ro 16-6028 and Ro 17-1812 produced responding on the drug lever. At a dose of 10 mg/kg both compounds gave rise to 100% responding on the lever associated with chlordiazepoxide. The dose-response curve produced by Ro 16-6028 was flatter than that for Ro 17-1812, however. The discriminative cue produced by 2 mg/kg zolpidem did not generalise to either Ro 16-6028 or Ro 17-1812. In contrast, both of those compounds antagonised the zolpidem cue and also antagonised the reduction in response rates produced by zolpidem. These results are consistent with previous findings that Ro 16-6028 and Ro 17-1812 may exert anxiolytic-like effects typical of benzodiazepines while antagonising the depressant actions of benzodiazepine receptor ligands. The results are also consistent with the suggestion that the discriminative cues produced by chlordiazepoxide and zolpidem may be mediated, at least partially, by activity at different sub-types of benzodiazepine receptors.
研究了两种具有混合激动剂和拮抗剂特性的新型苯二氮䓬Ro 16 - 6028和Ro 17 - 1812对训练用于区分氯氮卓或苯二氮䓬受体配体唑吡坦的大鼠的影响。在从生理盐水区分5mg/kg氯氮卓的大鼠中,Ro 16 - 6028和Ro 17 - 1812均使大鼠在药物杠杆上产生反应。在10mg/kg的剂量下,两种化合物均使与氯氮卓相关的杠杆上出现100%的反应。然而,Ro 16 - 6028产生的剂量 - 反应曲线比Ro 17 - 1812的更平缓。2mg/kg唑吡坦产生的辨别性线索未泛化至Ro 16 - 6028或Ro 17 - 1812。相反,这两种化合物均拮抗唑吡坦线索,并且还拮抗唑吡坦引起的反应率降低。这些结果与先前的发现一致,即Ro 16 - 6028和Ro 17 - 1812可能发挥苯二氮卓典型的抗焦虑样作用,同时拮抗苯二氮䓬受体配体的抑制作用。这些结果也与以下建议一致,即氯氮卓和唑吡坦产生的辨别性线索可能至少部分地由不同亚型苯二氮䓬受体的活性介导。