Phenethyl nicotinamides, a novel class of NaV1.7 channel blockers: Structure and activity relationship

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 19, 2012, Pages 6108-6115

  Kers, Inger ^a   MacSari, Istvan ^a   Csjernyik, Gabor ^a   Nylöf, Martin ^a   Skogholm, Karin ^a   Sandberg, Lars ^a   Minidis, Alexander ^a   Bueters, Tjerk ^a   Malmborg, Jonas ^a   Eriksson, Anders B ^a   Lund, Per Eric ^a   Venyike, Elisabet ^a   Luo, Lei ^a   Nyström, Jan Erik ^a   Besidski, Yevgeni ^a  

^a ASTRAZENECA R AND D   (Sweden)

Author keywords

NaV1.7 blocker; Pain; Phenethyl nicotinamides; Sodium channel blockers; Voltage gated channel

Indexed keywords

CARBAMAZEPINE; LAMOTRIGINE; LIDOCAINE; NICOTINIC ACID; PHENETHYL NICOTINAMIDE; PYRAZINE DERIVATIVE; SODIUM CHANNEL BLOCKING AGENT; SODIUM CHANNEL NAV1.5; SODIUM CHANNEL NAV1.7; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DEVELOPMENT; DRUG EFFICACY; DRUG MEGADOSE; DRUG METABOLISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; DRUG TRANSFORMATION; EX VIVO STUDY; FIRST PASS EFFECT; IC 50; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; LIVER MICROSOME METABOLISM; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PHARMACOKINETICS; PLASMA CONCENTRATION-TIME CURVE; RAT; STRUCTURE ACTIVITY RELATION; SUZUKI REACTION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MICROSOMES, LIVER; MOLECULAR STRUCTURE; NAV1.7 VOLTAGE-GATED SODIUM CHANNEL; NIACINAMIDE; RATS; SODIUM CHANNEL BLOCKERS; SOLUBILITY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84866350092     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.08.031     Document Type: Article

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