LY-255582

Modify Date: 2024-01-12 10:08:42

LY-255582 Structure
LY-255582 structure
Common Name LY-255582
CAS Number 119193-09-8 Molecular Weight 345.51900
Density N/A Boiling Point N/A
Molecular Formula C22H35NO2 Melting Point N/A
MSDS USA Flash Point N/A

 Use of LY-255582


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].

 Names

Name ly 255582
Synonym More Synonyms

 LY-255582 Biological Activity

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.  

 Chemical & Physical Properties

Molecular Formula C22H35NO2
Molecular Weight 345.51900
Exact Mass 345.26700
PSA 43.70000
LogP 4.26090

 Safety Information

RIDADR NONH for all modes of transport

 Precursor & DownStream

Precursor  1

DownStream  0

 Articles1

More Articles
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...

 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