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J Pharm Pharmacol. 1984 Dec;36(12):837-40. doi: 10.1111/j.2042-7158.1984.tb04888.x.
Ro 5-3663 is a convulsant 1,4-benzodiazepine that does not act at the benzodiazepine, but at the picrotoxin, site. To characterize the behavioural actions of Ro 5-3663, a comparison was made between its effects and those of picrotoxin, when combined with several compounds that act at the GABA-benzodiazepine receptor complex. The quinolines, PK 8165, PK 9084 and CGS 8216 caused myoclonic jerks when combined with subconvulsant doses of Ro 5-3663 or picrotoxin; in combination with picrotoxin they also caused full tonic-clonic convulsions. Ro 15-1788 (1, 10 mg kg-1) caused myoclonic jerks when it was given 10 min before, or at the same time as, subconvulsant doses of either compound. Diazepam (2, 4 mg kg-1) was anticonvulsant against both compounds. However, Ro 15-1788 (10, 20 mg kg-1, 20 min before), PK 8165 (80 mg kg-1) and PK 9084 (60 mg kg-1) were effective only against the convulsions induced by Ro 5-3663. It is not possible to determine whether these differences between Ro 5-3663 and picrotoxin are quantitative or qualitative.
Ro 5-3663是一种惊厥性1,4-苯二氮䓬类药物，它并非作用于苯二氮䓬类药物的作用位点，而是作用于印防己毒素的作用位点。为了明确Ro 5-3663的行为学作用，将其与印防己毒素的作用效果进行了比较，同时还比较了它们与几种作用于γ-氨基丁酸-苯二氮䓬受体复合物的化合物联合使用时的效果。喹啉类化合物PK 8165、PK 9084和CGS 8216与低于惊厥剂量的Ro 5-3663或印防己毒素联合使用时会引起肌阵挛性抽搐；与印防己毒素联合使用时还会引发全身性强直-阵挛性惊厥。Ro 15-1788（1、10 mg·kg⁻¹）在低于惊厥剂量的两种化合物给药前10分钟或同时给药时会引起肌阵挛性抽搐。地西泮（2、4 mg·kg⁻¹）对这两种化合物均有抗惊厥作用。然而，Ro 15-1788（10、20 mg·kg⁻¹，提前20分钟给药）、PK 8165（80 mg·kg⁻¹）和PK 9084（60 mg·kg⁻¹）仅对Ro 5-3663诱导的惊厥有效。无法确定Ro 5-3663和印防己毒素之间的这些差异是定量的还是定性的。
