Drug Discov Ther. 2007;1(1):45-56.

Anti-depressant and anti-nociceptive effects of 1,4-benzodiazepine-2-ones based cholecystokinin (CCK2) antagonists.

Lattmann E, Sattayasai J, Lattmann P, Billington DC, Schwalbe CH, Boonprakob J, Airarat W, Singh H, Offel M, Staaf A


Various 1,4-benzodiazepines were synthesized around a Diazepam, Oxazepam and the n-propyl-1,4-benzodiazepine template. SAR studies of CCK2 binding affinity were performed and selected examples of each series were tested in vivo in mice. In addition to an anxiolytic effect, antidepressant effects were discovered using 8 standard CNS assays in mice. Finally, the cocomittant administration of the 1,4-benzodiazepine based CCK antagonists enhanced the response to pain with a low dose of morphine, significantly.

KEYWORDS: 1,4-Benzodiazepine template, anxiolytics, antidepressant, anti-nociceptive agent, CCK-B antagonist, CCK2

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