Tetrahydroquinoline derivatives as opioid receptor antagonists.

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Zhang C, Westaway SM, Speake JD, Bishop MJ, Goetz AS, Carballo LH, Hu M, Epperly AH

Tetrahydroquinoline derivatives as opioid receptor antagonists.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):670-6. doi: 10.1016/j.bmcl.2010.12.010. Epub 2010 Dec 8.

PubMed ID

21193310 [ View in PubMed

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Abstract

Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58nM (K(i)) functional activity against the mu opioid receptor. DMPK data suggest that novel tetrahydroquinoline analogs may be advantageous in peripheral applications.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Naltrexone	Kappa-type opioid receptor	Ki (nM)	10	N/A	N/A	Details
Naltrexone	Mu-type opioid receptor	Ki (nM)	2	N/A	N/A	Details