Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.
Several novel racemic aminotetralin derivatives have been prepared using a stereoselective aziridine ring opening reactions and were evaluated for their micro-opioid receptor binding affinity. Selectivity index towards other opioid receptors and antinociceptive activity in mice have been evaluated for the most potent derivatives.
Roy
Caroline
C
Shire Biochem, 275 Armand-Frappier Blvd., Laval, H7V 4A7, Québec, Canada. croy@ca.shire.com
Li
Ticheao
T
Krasik
Pavel
P
Gilbert
Marie-Joseé
MJ
Pelletier
Christine
C
Gagnon
Diane
D
Robert
Ed
E
Ducharme
Julie
J
Storer
Richard
R
Lavallée
Jean-François
JF
D000701:Analgesics, Opioid / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D007202:Indicators and Reagents; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D017465:Receptors, Opioid, delta / Q000187:drug effects / Q000378:metabolism; D017473:Receptors, Opioid, kappa / Q000187:drug effects / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology*
D000701:Analgesics, Opioid; D007202:Indicators and Reagents; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D013764:Tetrahydronaphthalenes