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

Volumn 54, Issue 16, 2011, Pages 5868-5877

  Verhoest, Patrick R ^a   Sawant Basak, Aarti ^a   Parikh, Vinod ^a   Hayward, Matthew ^a   Kauffman, Gregory W ^a   Paradis, Vanessa ^a   McHardy, Stanton F ^a   McLean, Stafford ^a   Grimwood, Sarah ^a   Schmidt, Anne W ^a   Vanase Frawley, Michelle ^a   Freeman, Jodi ^a   Van Deusen, Jeffrey ^a   Cox, Loretta ^a   Wong, Diane ^a   Liras, Spiros ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 METHYL N [[2' (PYRROLIDIN 1 YLSULFONYL)BIPHENYL 4 YL]METHYL]PROPAN 1 AMINE; KAPPA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR ANTAGONIST; MONOMER; MORPHINE; PF 4455242; UNCLASSIFIED DRUG;

ANALGESIA; AREA UNDER THE CURVE; ARTICLE; DRUG CLEARANCE; DRUG DESIGN; DRUG EXPOSURE; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; HUMAN; NONHUMAN; PHYSICAL CHEMISTRY; STRUCTURE ACTIVITY RELATION; TAIL FLICK TEST;

3,4-DICHLORO-N-METHYL-N-(2-(1-PYRROLIDINYL)-CYCLOHEXYL)-BENZENEACETAMIDE, (TRANS)-ISOMER; ANALGESICS; ANIMALS; AREA UNDER CURVE; BIPHENYL COMPOUNDS; BRAIN; DISEASE MODELS, ANIMAL; DOGS; DRUG DESIGN; DRUG DISCOVERY; HAPLORHINI; HUMANS; METABOLIC CLEARANCE RATE; MICE; MICROSOMES, LIVER; MODELS, CHEMICAL; MOLECULAR STRUCTURE; MORPHINE; NARCOTIC ANTAGONISTS; PAIN; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, OPIOID, KAPPA; RECEPTORS, OPIOID, MU; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 80051865603     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2006035     Document Type: Article

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