L-152,804 是一种具有口服活性的选择性神经肽 Y Y5 受体 (NPY5-R) 拮抗剂，对 hY5 的 Ki 值为 26 nM。
L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure[1][2].
L 152804 displays > 300-fold selectivity over hY1, hY2, and hY4 receptors[1].
参考文献:
[1]. Kanatani A, et al. L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem Biophys Res Commun. 2000 May 27;272(1):169-73.
[2]. Mashiko S, et al. A pair-feeding study reveals that a Y5 antagonist causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure. Mol Pharmacol. 2007 Feb;71(2):602-8. Epub 2006 Nov 14.
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