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Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.

Roy, Caroline; Li, Ticheao; Krasik, Pavel; Gilbert, Marie-Joseé; Pelletier, Christine; Gagnon, Diane; Robert, Ed; Ducharme, Julie; Storer, Richard; Lavallée, Jean-François.

Bioorg Med Chem Lett ; 12(21): 3141-3, 2002 Nov 04.

Article in English | MEDLINE | ID: mdl-12372519

ABSTRACT

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.

Subject(s)

Analgesics, Opioid/chemical synthesis , Analgesics, Opioid/pharmacology , Receptors, Opioid, mu/drug effects , Tetrahydronaphthalenes/chemical synthesis , Tetrahydronaphthalenes/pharmacology , Animals , Indicators and Reagents , Mice , Pain Measurement/drug effects , Receptors, Opioid, delta/drug effects , Receptors, Opioid, delta/metabolism , Receptors, Opioid, kappa/drug effects , Receptors, Opioid, kappa/metabolism , Stereoisomerism , Structure-Activity Relationship

ABSTRACT

Subject(s)

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