4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective δ-opioid agonists with potential anxiolytic/antidepressant properties. Part 2

Novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives have been prepared and their synthesis described herein. In vitro affinities for δ-, μ-, and κ-opioid receptors are reported. Evaluation of some representative compounds from this series in the mouse neonatal ultrasonic vocalization test and the mouse tail suspension test revealed anxiolytic- and antidepressant-like effects, respectively, upon subcutaneous administration.

Graphical abstractSelective δ-opioid agonists based on the 4-phenyl-4-[1H-imidazol-2-yl]-piperidine scaffold are reported. Compound 3h has shown anxiolytic-/antidepressant-like effects in two mouse animal models.Figure optionsDownload full-size imageDownload as PowerPoint slide