4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective delta-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 delta-, micro-, and kappa-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.
Trabanco
Andrés A
AA
Johnson & Johnson Pharmaceutical Research & Development, Research & Early Development Europe, CNS-Psychiatry, Spain. atrabanc@prdes.jnj.com
Aerts
Nancy
N
Alvarez
Rosa M
RM
Andrés
José I
JI
Boeckx
Inge
I
Fernández
Javier
J
Gómez
Antonio
A
Janssens
Frans E
FE
Leenaerts
Joseph E
JE
De Lucas
Ana I
AI
Matesanz
Encarna
E
Steckler
Thomas
T
Pullan
Shirley
S
D014151:Anti-Anxiety Agents / Q000737:chemistry / Q000494:pharmacology*; D000928:Antidepressive Agents / Q000737:chemistry / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D017465:Receptors, Opioid, delta / Q000819:agonists*
C508741:4-phenyl-4-(1H-imidazol-2-yl)piperidine; D014151:Anti-Anxiety Agents; D000928:Antidepressive Agents; D010880:Piperidines; D017465:Receptors, Opioid, delta