PF-4455242 is a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor.[1][2] Discovered by Pfizer in 2009, it was pursued in a phase I clinical trial for the treatment of bipolar disorder,[3] and was also investigated as a treatment for depression and substance abuse.[4] However, development was stopped in September 2010 due to toxicology findings in animals that had been exposed to the drug for three months.[3]
See also
References
- ^ Verhoest PR, Basak AS, Parikh V, Hayward M, Kauffman GW, Paradis 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)". Journal of Medicinal Chemistry. 54 (16): 5868–5877. doi:10.1021/jm2006035. PMID 21744827.
- ^ Melief EJ, Miyatake M, Carroll FI, Béguin C, Carlezon WA, Cohen BM, 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". Molecular Pharmacology. 80 (5): 920–929. doi:10.1124/mol.111.074195. PMC 3198912. PMID 21832171.
- ^ a b Chaki S, Kanuma K (2012). "Neuropeptide Receptors: Novel Therapeutic Targets for Depression and Anxiety Disorders". In Rankovic Z, Hargreaves R, Bingham M (eds.). Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. pp. 314–317. ISBN 978-1-84973-365-6.
- ^ Goli V, Pryde D, Omoto K (2013). "Oral Opioids". In Allerton C, Fox D (eds.). Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. p. 50. ISBN 978-1-84973-645-9.