Bioorganic and Medicinal Chemistry Letters p. 6856 - 6860 (2011)
Update date:2022-07-30
Topics:
Yang, Yifan
Miller, Keith J.
Zhu, Yeheng
Hong, Yang
Tian, Yuan
Murugesan, Natesan
Gu, Zhengxiang
O'Tanyi, Eva
Keim, William J.
Rohrbach, Kenneth W.
Johnghar, Susan
Behnia, Kamelia
Pelleymounter, Mary Ann
Carlson, Kenneth E.
Ewing, William R.
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.
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Doi:10.1007/s00044-011-9849-0
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(2011)
