Bradwejn J, De Montigny C
Eur J Pharmacol. 1985 Jun 19;112(3):415-8. doi: 10.1016/0014-2999(85)90790-3.
Benzodiazepines (BZD) have been reported to suppress cholecystokinin-8S (CCK-8S)-induced activation. PK 8165, a ligand of BZD receptors, is an anxiolytic devoid of sedative and anticonvulsant effects. PK 8165, applied microiontophoretically or administered i.v. at low doses, suppressed CCK-8S-induced activation of hippocampal pyramidal neurons, whereas, at high doses it antagonized the effect of microiontophoretic applications of flurazepam. These results indicate that PK 8165 acts as a mixed agonist-antagonist at BZD receptors and suggest that the suppression of CCK-8S-induced activation by BZD might be related to their anxiolytic property rather than to their sedative or anticonvulsant activity.
据报道，苯二氮䓬类药物（BZD）可抑制胆囊收缩素-8S（CCK-8S）诱导的激活。PK 8165是一种BZD受体配体，是一种无镇静和抗惊厥作用的抗焦虑药。以微量离子透入法应用或静脉注射低剂量的PK 8165，可抑制CCK-8S诱导的海马锥体神经元激活，而高剂量时它可拮抗微量离子透入法应用氟西泮的作用。这些结果表明，PK 8165在BZD受体上起混合激动剂-拮抗剂的作用，并提示BZD对CCK-8S诱导激活的抑制作用可能与其抗焦虑特性有关，而非与其镇静或抗惊厥活性有关。
