|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||372.53 g·mol−1|
|3D model (JSmol)|
PF-4455242 is a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor. Discovered by Pfizer in 2009, it was pursued in a phase I clinical trial for the treatment of bipolar disorder, and was also investigated as a treatment for depression and substance abuse. However, development was stopped in September 2010 due to toxicology findings in animals that had been exposed to the drug for three months.
- Verhoest PR, Basak AS, Parikh V, et al. (August 2011). "Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242)". J. Med. Chem. 54 (16): 5868–77. doi:10.1021/jm2006035. PMID 21744827.
- Melief EJ, Miyatake M, Carroll FI, et al. (November 2011). "Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation". Mol. Pharmacol. 80 (5): 920–9. doi:10.1124/mol.111.074195. PMC 3198912. PMID 21832171.
- 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.
- Charlotte Allerton; David Fox (2013). Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. p. 50. ISBN 978-1-84973-645-9.
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