3-oxoisoindoline-1-carboxamides: Potent, state-dependent blockers of voltage-gated sodium channel na v1.7 with efficacy in rat pain models

Journal of Medicinal Chemistry

Volumn 55, Issue 15, 2012, Pages 6866-6880

  MacSari, Istvan ^a   Besidski, Yevgeni ^a   Csjernyik, Gabor ^a   Nilsson, Linda I ^a   Sandberg, Lars ^a   Yngve, Ulrika ^a   Åhlin, Kristofer ^a   Bueters, Tjerk ^a   Eriksson, Anders B ^a   Lund, Per Eric ^a   Venyike, Elisabet ^a   Oerther, Sandra ^a   Hygge Blakeman, Karin ^a   Luo, Lei ^a   Arvidsson, Per I ^a,b,c  

^a ASTRAZENECA R AND D   (Sweden)

^b UPPSALA UNIVERSITY   (Sweden)

^c UNIVERSITY OF KWAZULU NATAL   (South Africa)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4,4 DIFLUOROCYCLOHEXYL) 3 OXO N [4 (TRIFLUOROMETHOXY)BENZYL]ISOINDOLINE 1 CARBOXAMIDE; 2 (OXAN 4 YL) 3 OXO N [[4 (TRIFLUOROMETHOXY)PHENYL]METHYL] 1H ISOINDOLE 1 CARBOXAMIDE; 2 [2 (5 FLUOROPYRIMIDIN 2 YL)ETHYL] 3 OXO N [3 (TRIFLUOROMETHOXY)BENZYL]ISOINDOLINE 1 CARBOXAMIDE; 2 [2 (5 FLUOROPYRIMIDIN 2 YL)ETHYL] 3 OXO N [4 (TRIFLUOROMETHOXY)BENZYL]ISOINDOLINE 1 CARBOXAMIDE; 3 OXO 2 (2 PYRIDIN 2 YLETHYL) N [[4 (TRIFLUOROMETHOXY)PHENYL]METHYL] 1H ISOINDOLE 1 CARBOXAMIDE; 3 OXOISOINDOLINE 1 CARBOXAMIDE DERIVATIVE; AMITRIPTYLINE; ISOINDOLE DERIVATIVE; N (3,4 DIMETHYLPHENYL) 3 OXO 2 [2 (PYRIDIN 2 YL)ETHYL]ISOINDOLINE 1 CARBOXAMIDE; N [4 FLUORO 3 (TRIFLUOROMETHYL)BENZYL] 2 [2 (5 FLUOROPYRIMIDIN 2 YL)ETHYL] 3 OXOISOINDOLINE 1 CARBOXAMIDE; SODIUM CHANNEL BLOCKING AGENT; SODIUM CHANNEL NAV1.7; TETRACAINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BINDING SITE; CONTROLLED STUDY; DISTRIBUTION VOLUME; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; MALE; MAXIMUM PLASMA CONCENTRATION; NOCICEPTION; NONHUMAN; NUCLEOTIDE SEQUENCE; PAIN; RAT; SPINAL GANGLION; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

AMIDES; ANALGESICS; ANIMALS; ARTHRITIS, EXPERIMENTAL; CARRAGEENAN; CHO CELLS; CHRONIC PAIN; CRICETINAE; CRICETULUS; HEK293 CELLS; HUMANS; ISOINDOLES; MALE; MICROSOMES, LIVER; PAIN; PATCH-CLAMP TECHNIQUES; RATS; RATS, SPRAGUE-DAWLEY; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; SOLUBILITY; SPINAL NERVES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84864949618     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300623u     Document Type: Article

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