8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.
A series of 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan+ ++-4-one derivatives 1 was studied with respect to the binding affinity for the orphanin FQ (OFQ) and opioid (mu, kappa, delta) receptors. The influence of stereochemistry as well as the substitution pattern of the phenyl-ring in position 1 on the affinity for the orphanin FQ receptor and selectivity to opioid (mu, kappa, delta) receptors is discussed. The most interesting compound 1c was tested for its anxiolytic-like properties in vivo.
Wichmann
J
J
Pharma Division, Preclinical CNS Research, F. Hoffmann-La Roche Ltd, Basel. juergen.wichmann@roche.com
Adam
G
G
Röver
S
S
Cesura
A M
AM
Dautzenberg
F M
FM
Jenck
F
F
D000818:Animals; D014151:Anti-Anxiety Agents / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D006224:Cricetinae; D005106:Exploratory Behavior / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D011957:Receptors, Opioid / Q000819:agonists*; D013141:Spiro Compounds / Q000737:chemistry / Q000494:pharmacology*; D000094942:Nociceptin Receptor
C121726:8-acenaphthen-1-yl-1-phenyl-1,3,8-triazaspiro(4.5)decan-4-one; D014151:Anti-Anxiety Agents; D007093:Imidazoles; D011957:Receptors, Opioid; D013141:Spiro Compounds; D000094942:Nociceptin Receptor