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

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Roy C, Li T, Krasik P, Gilbert MJ, Pelletier C, Gagnon D, Robert E, Ducharme J, Storer R, Lavallee JF

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

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3141-3.

PubMed ID

12372519 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Morphine	Kappa-type opioid receptor	Ki (nM)	52.14	N/A	N/A	Details
Morphine	Mu-type opioid receptor	Ki (nM)	3.96	N/A	N/A	Details