119193-09-8

119193-09-8 structure
119193-09-8 structure
  • Name: LY-255582
  • Chemical Name: ly 255582
  • CAS Number: 119193-09-8
  • Molecular Formula: C22H35NO2
  • Molecular Weight: 345.51900
  • Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
  • Create Date: 2017-09-04 01:18:11
  • Modify Date: 2024-01-12 10:08:42
  • LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity[1][2][3][4].

Name ly 255582
Synonyms (+)-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
Description LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity[1][2][3][4].
Related Catalog
Target

μ Opioid Receptor/MOR:0.4 nM (Ki)

δ Opioid Receptor/DOR:5.2 nM (Ki)

κ Opioid Receptor/KOR:2.0 nM (Ki)

In Vitro LY255582 (40 μM, 24-72 h) 抑制 Huh7 和 MHCC-97H 细胞活力[5]。
In Vivo LY255582 (100 μg,i.c.v.) 减少大鼠的食物摄入量[1]。 LY255582 (15 mg/kg,皮下注射,每日一次) 减少喂食的肥胖 Zucker 大鼠的食物摄入量和体重增加[4]。 Animal Model: STZ-induced diabetic mice[1] Dosage: 100, 10 and 1 μg Administration: i.c.v. Result: Decreased food at 100, 10 and 1 μg by 76, 62 and 29%.
References

[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.  

Molecular Formula C22H35NO2
Molecular Weight 345.51900
Exact Mass 345.26700
PSA 43.70000
LogP 4.26090
RIDADR NONH for all modes of transport
Precursor  1

DownStream  0