Translational gaps on the psychiatry/analgesic potential of CCK2r antagonists
| Preclinical evidence | Clinical trials | ||||
|---|---|---|---|---|---|
| Compound (dosage) length | Outcomes | References | Compound (dosage) length | Outcomes | References |
| CI-988 (0.001–10.0 mg/kg, i.p.)Acute | Anxiolytic-like action in rats elevated the X-maze, rat social interaction test, and mouse light/dark shuttle box | [208] | CI-988 (300 mg/day, thrice daily)Four weeks | No anxiolytic effect in general anxiety disorder | [23] |
| CI-988 (100 mg/day, thrice daily)Six weeks | No anxiolytic effect in panic disorder | [25] | |||
| L-365,260 (3.2, 10, and 32 mg/kg, i.p.)Acute | Antipanic-like effects in rats receiving brain stimulation in the dorsal PAG | [209] | L-365,260 (30 mg/day, four times daily)Six weeks | No anxiolytic effect in panic disorder | [24] |
| CI-988 and L-365,260 (8.9, 0.16, and 0.25 μmol/kg, i.p.)Acute | Anxiolytic-like action in rats elevated the X-maze | [210] | L-365,260 (10–50 mg)Acute | CCK-4 panicogenic effects are antagonized by L-365,260 in panic disorder patients | [211] |
| L-365,260 (0.1 and 0.5 mg/kg, s.c.)Acute | Enhancement of the analgesia induced by a submaximal dose of morphine | [212] | L-365,260 (10 mg and 40 mg thrice daily)Two weeks | L-365,260 fails to augment morphine-induced analgesia in chronic neuropathic pain | [26] |
i.p.: intraperitoneal; s.c.: subcutaneous. PAG: periaqueductal grey; CCK-4: cholecystokinin tetrapeptide
SJB: Conceptualization, Investigation, Methodology, Validation, Writing—original draft, Writing—review & editing.
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Santiago J. Ballaz, who is the Guest Editor of Exploration of Drug Science, had no involvement in the decision-making or the review process of this manuscript.
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