Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain

Journal of Medicinal Chemistry

Volumn 54, Issue 13, 2011, Pages 4427-4445

  Bregman, Howard ^a   Berry, Loren ^a   Buchanan, John L ^a   Chen, April ^a   Du, Bingfan ^a   Feric, Elma ^a   Hierl, Markus ^a   Huang, Liyue ^a   Immke, David ^b   Janosky, Brett ^a   Johnson, Danielle ^a   Li, Xingwen ^a   Ligutti, Joseph ^b   Liu, Dong ^b   Malmberg, Annika ^a   Matson, David ^a   McDermott, Jeff ^a   Miu, Peter ^b   Nguyen, Hanh Nho ^a   Patel, Vinod F ^a   Waldon, Daniel ^a   Wilenkin, Ben ^a   Zheng, Xiao Mei ^a   Zou, Anruo ^b   McDonough, Stefan I ^a   Dimauro, Erin F ^a   more..

^a AMGEN INC   (United States)

^b Department of Lead Discovery ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (4 (3 ACETAMIDOPHENYLAMINO) 1,3,5 TRIAZIN 2 YL)PIPERIDINE 4 CARBOXAMIDE; 2,4 TRIAZINEDIAMINE DERIVATIVE; N (2 METHYL 3 (4 (4 (1 PHENYLETHOXY)PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (2 METHYL 3 (4 (4 (4 (TRIFLUOROMETHOXY)BENZYLOXY) PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (2 METHYL 3 (4 (4 (4 (TRIFLUOROMETHOXY)BENZYLOXY)PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (2 METHYL 3 (4 (4 (4 (TRIFLUOROMETHYL)BENZYLOXY)PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (2 METHYL 3 (4 (4 (4 (TRIFLUOROMETHYL)PHENOXY)PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (2 METHYL 3 (4 (4 PHENOXYPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (2 METHYL 3 (4 (4 PHENYLPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (3 (2 (3,4 DIHYDROISOQUINOLIN 2(1H) YL)PYRIMIDIN 4 YLAMINO)PHENYL)ACETAMIDE; N (3 (4 (3,4 DIHYDROISOQUINOLIN 2(1H) YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (3 (4 (3,4 DIHYDROISOQUINOLIN 2(1H) YL) 1,3,5 TRIAZIN 2 YLOXY)PHENYL)ACETAMIDE; N (3 (4 (3,4 DIHYDROISOQUINOLIN 2(1H) YL)PYRIMIDIN 2 YLAMINO)PHENYL)ACETAMIDE; N (3 (4 (4 (BENZYLOXY)PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) 2 METHYLPHENYL)ACETAMIDE; N (3 (4 (4 (BENZYLOXY)PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) PHENYL)ACETAMIDE; N (3 (4 (4 BENZOYLPIPERAZIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) PHENYL)ACETAMIDE; N (3 (4 (4 BENZYLPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) PHENYL)ACETAMIDE; N (3 (4 (4 HYDROXY 4 PHENYLPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (3 (4 (4 METHOXYPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) PHENYL)ACETAMIDE; N (3 (4 (4 METHYLPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) PHENYL)ACETAMIDE; N (3 (4 (4 PHENOXYPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) PHENYL)ACETAMIDE; N (3 (4 (4 PHENYLPIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO) PHENYL)ACETAMIDE; N (3 (4 (PIPERIDIN 1 YL) 1,3,5 TRIAZIN 2 YLAMINO)PHENYL) ACETAMIDE; N (3 (4 AMINO 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (3 (4 CHLORO 1,3,5 TRIAZIN 2 YLAMINO) 2 METHYLPHENYL) ACETAMIDE; N (3 (4 CHLORO 1,3,5 TRIAZIN 2 YLAMINO)PHENYL)ACETAMIDE; N (3 (6 (3,4 DIHYDROISOQUINOLIN 2(1H) YL)PYRIMIDIN 4 YLAMINO)ACETAMIDE; N (3 [(4 (3,4 DIHYDROISOQUINOLIN 2(1H) YL) 1,3,5 TRIAZIN 2 YL)(METHYL)AMINO)PHENYL]ACETAMIDE; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING SITE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE INCREASE; DRUG MECHANISM; DRUG POTENCY; DRUG SOLUBILITY; DRUG STRUCTURE; IN VIVO STUDY; MALE; NONHUMAN; PAIN; RAT; SENSORY NERVE CELL; STRUCTURE ACTIVITY RELATION;

ACETAMIDES; ADMINISTRATION, ORAL; ANALGESICS; ANIMALS; BINDING SITES; CELL LINE; ETHER-A-GO-GO POTASSIUM CHANNELS; FORMALDEHYDE; GANGLIA, SPINAL; HUMANS; MICROSOMES, LIVER; NERVE TISSUE PROTEINS; NEURONS; PAIN; PAIN MEASUREMENT; PATCH-CLAMP TECHNIQUES; RATS; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; TETRODOTOXIN; TRIAZINES;

EID: 79960186294     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200018k     Document Type: Article

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