Purity: > 98%
PF-4455242(cas 1322001-35-3) is a selective, short-acting antagonist of the κ-opioid receptor. 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.
1:J Med Chem. 2011 Aug 25;54(16):5868-77. doi: 10.1021/jm2006035. Epub 2011 Jul 22. 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).Verhoest PR,Basak AS,Parikh V,Hayward M,Kauffman GW,Paradis V,McHardy SF,McLean S,Grimwood S,Schmidt AW,Vanase-Frawley M,Freeman J,Van Deusen J,Cox L,Wong D,Liras S, PMID: 21744827 DOI: 10.1021/jm2006035
Abstract: By use of parallel chemistry coupled with physicochemical property design, a series of selective κ opioid antagonists have been discovered. The parallel chemistry strategy utilized key monomer building blocks to rapidly expand the desired SAR space. The potency and selectivity of the in vitro κ antagonism were confirmed in the tail-flick analgesia model. This model was used to build an exposure-response relationship between the κ K(i) and the free brain drug levels. This strategy identified 2-methyl-N-((2/'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242, which entered phase 1 clinical testing and has demonstrated target engagement in healthy volunteers.© 2011 American Chemical Society