LY255582

≥98% (HPLC)

Synonym: (3R,4R)-3,4-Dimethyl-1-[(3S)-3-hydroxy-3-cyclohexyl-propyl]-4-(3-hydroxyphenyl)piperidine, (aS,3R,4R)-a-Cyclohexyl-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinepropanol, LY-255582

CAS Number 119193-09-8
Empirical Formula (Hill Notation) C₂₂H₃₅NO₂
Molecular Weight 345.52
MDL number MFCD00878181

Properties

Related Categories	Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology, Cell Signaling and Neuroscience, Eli Lilly, Excitatory Amino Acids - Opiod Antagonists, GPCR Modulators, GPCR Proteins, Modulators and Antibodies, L, Membrane Protein Biology Tools, Neurobiology, Neuroscience, Opioid Antagonists, Opioids, Pharmacologicals, Proteins and Derivatives More...
assay	≥98% (HPLC)
form	powder
storage condition	desiccated
color	white to beige
solubility	DMSO: ≥15 mg/mL
storage temp.	2-8°C

Description

Biochem/physiol Actions

LY255582 is a centrally active opioid receptor antagonist (defined as an inverse agonist in 2011 JPET paper) that inhibited weight gain in obese Zucker rats over 30 days. It is more that 5-fold selective for mu opioid receptor compared to kappa opioid receptors and 13-fold selective over delta opioid receptors.

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Papers

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Activation of mesolimbic dopamine neurons during novel and daily limited access to palatable food is blocked by the opioid antagonist LY255582. Sahr AE, Sindelar DK, Alexander-Chacko JT, Eastwood BJ, Mitch CH, Statnick MA. Am. J. Physiol. Regul. Integr. Comp. Physiol. 2, R463-71, (2008)

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. Need AB, McKinzie JH, Mitch CH, Statnick MA, Phebus LA. Life Sci. 17-18, 1389-96, (2007)

SAR and biological evaluation of novel trans-3,4-dimethyl-4-arylpiperidine derivatives as opioid antagonists. Díaz N, Benvenga M, Emmerson P, Favors R, Mangold M, McKinzie J, et al. Bioorg. Med. Chem. Lett. 17, 3844-8, (2005)

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