|Related Categories||Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology, Cell Signaling and Neuroscience,|
|color||white to beige|
|solubility||DMSO: ≥15 mg/mL|
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.
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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