Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.

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Yang Y, Miller KJ, Zhu Y, Hong Y, Tian Y, Murugesan N, Gu Z, O'Tanyi E, Keim WJ, Rohrbach KW, Johnghar S, Behnia K, Pelleymounter MA, Carlson KE, Ewing WR

Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6856-60. doi: 10.1016/j.bmcl.2011.09.016. Epub 2011 Sep 13.

PubMed ID

21962575 [ View in PubMed

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Abstract

Obesity remains a significant public health issue leading to Type II diabetes and cardiovascular disease. CB1 antagonists have been shown to suppress appetite and reduce body weight in animal models as well as in humans. Evaluation of pre-clinical CB1 antagonists to establish relationships between in vitro affinity and in vivo efficacy parameters are enhanced by ex vivo receptor occupancy data. Synthesis and biological evaluation of a novel and highly selective radiolabeled CB1 antagonist is described. The radioligand was used to conduct ex vivo receptor occupancy studies.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rimonabant	Cannabinoid receptor 1	Ki (nM)	0.73	N/A	N/A	Details