Bennett D A
Research Department, Ciba-Geigy Corporation, Summit, NJ 07901.
Physiol Behav. 1987;41(3):241-5. doi: 10.1016/0031-9384(87)90360-x.
Five compounds that bind to the benzodiazepine (BZ) receptor, but show different pharmacological characteristics from the classical BZs, are profiled. CGS 8216 is a BZ antagonist/inverse agonist that reverses the effects of diazepam and also acts as a proconvulsant. CGS 9895 is also a potent BZ antagonist. In addition, this compound shows an anxiolytic profile. CGS 9896, CGS 17867A and CGS 20625 are BZ agonists (i.e., anxiolytics and anticonvulsants) which produce varying magnitudes of antagonist effect. All of these compounds are unique from the classical BZs in that each has a reduced propensity to produce the sedative and/or muscle relaxant effects characteristically associated with BZs.
对五种与苯二氮䓬（BZ）受体结合，但具有与经典苯二氮䓬不同药理特性的化合物进行了分析。CGS 8216是一种BZ拮抗剂/反向激动剂，可逆转地西泮的作用，并且还具有惊厥诱发作用。CGS 9895也是一种强效BZ拮抗剂。此外，该化合物具有抗焦虑特性。CGS 9896、CGS 17867A和CGS 20625是BZ激动剂（即抗焦虑药和抗惊厥药），它们产生不同程度的拮抗作用。所有这些化合物与经典苯二氮䓬不同，因为每种化合物产生与苯二氮䓬相关的镇静和/或肌肉松弛作用的倾向均降低。
