8-(Heteroaryl)phenalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as opioid receptor modulators.
A series of N-biarylalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones were prepared and evaluated for biological activity at opioid (mu, delta, kappa) and opioid receptor like-1 (ORL-1) G-protein coupled receptors. Substitution on the biaryl moiety produced enhanced affinity for the mu-opioid receptor.
Jordan
Alfonzo D
AD
Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, P.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA. ajordan@prdus.jnj.com
Orsini
Michael J
MJ
Middleton
Steven A
SA
Connolly
Peter J
PJ
Brenneman
Douglas E
DE
Pan
Kevin
K
Reitz
Allen B
AB
D000818:Animals; D001665:Binding Sites; D016466:CHO Cells; D002460:Cell Line; D002462:Cell Membrane / Q000187:drug effects; D006224:Cricetinae; D006801:Humans; D015394:Molecular Structure; D011957:Receptors, Opioid / Q000187:drug effects*; D013134:Spiperone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D011957:Receptors, Opioid; D013134:Spiperone