| 词条 | PF-4455242 |
| 释义 |
| IUPAC_name = 2-Methyl-N[2’-(1-pyrrolidinylsulfonyl)-4-biphenylyl]methyl1-propanamine | image = PF-4455242.svg | width = 250 | CAS_number = 1202647-54-8 | ATC_prefix = None | ATC_suffix = | PubChem = 44599828 | DrugBank = | ChemSpiderID = 26610764 | C=21 | H=28 | N=2 | O=2 | S=1 | molecular_weight = 372.524 g/mol | smiles = CC(C)CNCC1=CC=C(C=C1)C2=CC=CC=C2S(=O)(=O)N3CCCC3 | StdInChI = 1S/C21H28N2O2S/c1-17(2)15-22-16-18-9-11-19(12-10-18)20-7-3-4-8-21(20)26(24,25)23-13-5-6-14-23/h3-4,7-12,17,22H,5-6,13-16H2,1-2H3 | StdInChIKey = OWVIKBRKPCTDEP-UHFFFAOYSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Oral }}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
References1. ^{{cite journal |vauthors=Verhoest PR, Basak AS, Parikh V, etal | title = 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 = J. Med. Chem. | volume = 54 | issue = 16 | pages = 5868–77 |date=August 2011 | pmid = 21744827 | doi = 10.1021/jm2006035 | url = }} 2. ^{{cite journal |vauthors=Melief EJ, Miyatake M, Carroll FI, etal | title = Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation | journal = Mol. Pharmacol. | volume = 80 | issue = 5 | pages = 920–9 |date=November 2011 | pmid = 21832171 | pmc = 3198912 | doi = 10.1124/mol.111.074195 | url = }} 3. ^1 {{cite book | author1 = Zoran Rankovic | author2 = Richard Hargreaves | author3 = Matilda Bingham | title = Drug Discovery for Psychiatric Disorders | url = https://books.google.com/books?id=J4Mq3Lm1R7kC&pg=PA314 | year = 2012 | publisher = Royal Society of Chemistry | isbn = 978-1-84973-365-6 | pages = 314–317}} 4. ^{{cite book | author1 = Charlotte Allerton | author2 = David Fox | title = Pain Therapeutics: Current and Future Treatment Paradigms | url = https://books.google.com/books?id=zUINAgAAQBAJ&pg=PA50 | year = 2013 | publisher = Royal Society of Chemistry | isbn = 978-1-84973-645-9 | page = 50}} External links
4 : Amines|Kappa antagonists|Pyrrolidines|Sulfones |
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