Aminopyrazine CB1 receptor inverse agonists.

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Wustrow DJ, Maynard GD, Yuan J, Zhao H, Mao J, Guo Q, Kershaw M, Hammer J, Brodbeck RM, Near KE, Zhou D, Beers DS, Chenard BL, Krause JE, Hutchison AJ

Aminopyrazine CB1 receptor inverse agonists.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3376-81. doi: 10.1016/j.bmcl.2008.04.022. Epub 2008 Apr 13.

PubMed ID

18448340 [ View in PubMed

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Abstract

A series of 5,6-diaryl-2-amino-pyrazines were prepared and found to have antagonist-like properties at the CB1 receptor. Subsequent SAR studies optimized both receptor potency and drug-like properties including solubility and Cytochrome-P450 inhibition potential. Optimized compounds were demonstrated to be inverse agonists and compared in vivo with rimonabant for their ability to inhibit food intake, to occupy central CB1 receptors and to influence hormonal markers associated with obesity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rimonabant	Cannabinoid receptor 1	IC 50 (nM)	1.35	N/A	N/A	Details
Rimonabant	Cannabinoid receptor 1	Ki (nM)	0.43	N/A	N/A	Details