LY-255582

• 常用名: LY-255582
• 英文名: LY-255582
• CAS号: 119193-09-8
• 分子量: 345.51900
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₂H₃₅NO₂
• 熔点: N/A
• 闪点: N/A

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]。

LY-255582名称

• 英文名: ly 255582

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
• 靶点实验:

  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
• InChIKey: LVVHEFJXPXAUDD-BULFRSBZSA-N
• SMILES: CC1CN(CCC(O)C2CCCCC2)CCC1(C)c1cccc(O)c1

LY-255582安全信息

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

LY-255582靶点实验

查看更多实验

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu... 来源：NCGC External Id：CYP2C9536

实验名称：Inhibition of binding of [3H]DADLE to Opioid receptor delta 1 in guinea pig membranes 来源：ChEMBL 靶标：Delta-type opioid receptor External Id：CHEMBL755203

实验名称：qHTS assay to identify novel small-molecules to repurpose for Merkel cell carcinoma t... 来源：NCGC 靶标：N/A External Id：MCC011

实验名称：Primary qHTS for Identification of Calcium Integrin Binding Protein 1 (CIB1) Competit... 来源：NCGC External Id：CIB1-p1-p2

实验名称：Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screeni... 来源：NCGC 靶标：N/A External Id：CPF001

实验名称：The compound was tested for antagonist activity by selective inhibition of [35S]GTP-g... 来源：ChEMBL 靶标：Delta-type opioid receptor External Id：CHEMBL755878

实验名称：Antagonist activity at cloned human mu opioid receptor expressed in CHO cells assesse... 来源：ChEMBL 靶标：Mu-type opioid receptor External Id：CHEMBL901092

共68条，当前第1页，共7页

1

2

3

4

5

LY-255582英文别名

• (+)-1-[(3S)-3-Hydroxy-3-cyclohexylpropyl]-(3R,4R)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine
• (+)-1-(3(S)-3-hydroxy-3-cyclohexylpropyl)-3(R),4(R)-dimethyl-4-(3-hydroxyphenyl)piperidine