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Systematic (IUPAC) name
Clinical data
Legal status
Routes Oral
Pharmacokinetic data
Half-life 30–40 hours
CAS number 1174130-61-0
ATC code None
ChemSpider 28424203
Chemical data
Formula C26H27FN2O2 
Mol. mass 418.503 g/mol

LY-2456302 is a selective, short-acting antagonist of the κ-opioid receptor.[1][2] It is under development by Eli Lily as an augmentation to antidepressant therapy for treatment-resistant depression, and is currently in phase II clinical trials in the United States.[3][4] In animal models of depression, LY-2456302 has been found to have potent synergistic efficacy in combination with other antidepressants such as citalopram and imipramine.[4]

See also[edit]


  1. ^ Rorick-Kehn LM, Witkin JM, Statnick MA, et al. (February 2014). "LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders". Neuropharmacology 77: 131–44. doi:10.1016/j.neuropharm.2013.09.021. PMID 24071566. 
  2. ^ Lowe SL, Wong CJ, Witcher J, et al. (March 2014). "Safety, Tolerability, and Pharmacokinetic Evaluation of Single- and Multiple-Ascending Doses of a Novel Kappa Opioid Receptor Antagonist LY2456302 and Drug Interaction With Ethanol in Healthy Subjects". J Clin Pharmacol. doi:10.1002/jcph.286. PMID 24619932. 
  3. ^ Zoran Rankovic; Richard Hargreaves; Matilda Bingham (2012). Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. pp. 314–317. ISBN 978-1-84973-365-6. 
  4. ^ a b Urbano M, Guerrero M, Rosen H, Roberts E (May 2014). "Antagonists of the kappa opioid receptor". Bioorg. Med. Chem. Lett. 24 (9): 2021–32. doi:10.1016/j.bmcl.2014.03.040. PMID 24690494.