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  • Title: Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.
    Author: Matthews JM, McNally JJ, Connolly PJ, Xia M, Zhu B, Black S, Chen C, Hou C, Liang Y, Tang Y, Macielag MJ.
    Journal: Bioorg Med Chem Lett; 2016 Nov 01; 26(21):5346-5349. PubMed ID: 27671496.
    Abstract:
    A series of potent and receptor-selective cannabinoid-1 (CB1) receptor inverse agonists has been discovered. Peripheral selectivity of the compounds was assessed by a mouse tissue distribution study, in which the concentrations of a test compound in both plasma and brain were measured. A number of peripherally selective compounds have been identified through this process. Compound 2p was further evaluated in a 3-week efficacy study in the diet-induced obesity (DIO) mouse model. Beneficial effects on plasma glucose were observed from the compound-treated mice.
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