LY-255582

LY-255582用途

LY255582是一种泛阿片类拮抗剂,对μ、δ和κ受体具有高亲和力(Ki:0.4nM、5.2、2.0nM)。LY255582可以减少食物摄入量和体重。LY255582可用于肥胖的研究[1][2][3][4]。

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LY-255582名称

[ CAS 号 ]:
119193-09-8

[ 英文名 ]:
LY-255582

[英文别名 ]:

LY-255582生物活性

[ 描述 ]:

LY255582是一种泛阿片类拮抗剂,对μ、δ和κ受体具有高亲和力(Ki:0.4nM、5.2、2.0nM)。LY255582可以减少食物摄入量和体重。LY255582可用于肥胖的研究[1][2][3][4]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

研究领域 >> 代谢疾病

信号通路 >> 神经信号通路 >> 阿片受体

[ 靶点 ]

μ Opioid Receptor/MOR:0.4 nM (Ki)

δ Opioid Receptor/DOR:5.2 nM (Ki)

κ Opioid Receptor/KOR:2.0 nM (Ki)

[体外研究]

LY255582(40μM,24-72小时)抑制第七季度和 MHCC-97小时细胞活力[5]。

[体内研究]

LY255582(100μg,静脉注射)减少大鼠的食物摄入量[1]。 LY255582(15mg/kg皮下注射,每日一次) 减少喂食的肥胖祖克大鼠的食物摄入量和体重增加[4]。动物模型：STZ诱导的糖尿病小鼠[1]剂量：100、10和1μg给药：静脉注射。

[参考文献]

[1]. Levine AS, et al. Central administration of the opioid antagonist, LY255582, decreases short- and long-term food intake in rats. Brain Res. 1991 Dec 6;566(1-2):193-7.

[2]. Need AB, et al. In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously. Life Sci. 2007 Oct 13;81(17-18):1389-96.

[3]. S.L. Gackenheimer, et al. Localization of opioid receptor antagonist [3H]-LY255582 binding sites in mouse brain: Comparison with the distribution of mu, delta and kappa binding sites. Neuropeptides. 2005. 39 (6), 559-567.

[4]. Shaw WN, et al. Long-term treatment of obese Zucker rats with LY255582 and other appetite suppressants. Pharmacol Biochem Behav. 1993 Nov;46(3):653-9.

[5]. Chen DT, et al. The mu-opioid receptor is a molecular marker for poor prognosis in hepatocellular carcinoma and represents a potential therapeutic target. Br J Anaesth. 2019 Jun;122(6):e157-e167.

LY-255582物理化学性质

[ 分子式 ]:
C₂₂H₃₅NO₂

[ 分子量 ]:
345.51900

[ 精确质量 ]:
345.26700

[ PSA ]:
43.70000

[ LogP ]:
4.26090

LY-255582安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

LY-255582合成路线

详细合成路线

LY-255582上下游产品

LY-255582上游产品

LY-255582下游产品

LY-255582文献

Activation of mesolimbic dopamine neurons during novel and daily limited access to palatable food is blocked by the opioid antagonist LY255582.

Am. J. Physiol. Regul. Integr. Comp. Physiol. 295(2) , R463-71, (2008)

An analog of the trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine series (LY255582) exhibits high in vitro binding affinity and antagonist potency for the mu-, delta-, and kappa-opioid receptors. In v...

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