Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat

Journal of Medicinal Chemistry

Volumn 55, Issue 16, 2012, Pages 7114-7140

  Huber, John D ^a   Bentzien, Jörg ^a   Boyer, Stephen J ^a,d   Burke, Jennifer ^a   De Lombaert, Stéphane ^a,e   Eickmeier, Christian ^b   Guo, Xin ^a   Haist, James V ^c   Hickey, Eugene R ^a   Kaplita, Paul ^a,f   Karmazyn, Morris ^c   Kemper, Raymond ^a,g   Kennedy, Charles A ^a   Kirrane, Thomas ^a   Madwed, Jeffrey B ^a,h   Mainolfi, Elizabeth ^a   Nagaraja, Nelamangara ^a   Soleymanzadeh, Fariba ^a   Swinamer, Alan ^a   Eldrup, Anne B ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

^c UNIVERSITY OF WESTERN ONTARIO   (Canada)

^d BRISTOL MYERS SQUIBB   (United States)

^e Karos Pharmaceuticals   (United States)

^f MASSACHUSETTS COLLEGE OF PHARMACY AND HEALTH SCIENCES   (United States)

^g HOFFMANN LA ROCHE INC   (United States)

^h MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARIPORIDE; CYTOCHROME P450; CYTOCHROME P450 3A4; ENIPORIDE; ION CHANNEL; N [4 (1 ACETYLPIPERIDIN 4 YL) 3 TRIFLUOROMETHYLBENZOYL]GUANIDINE; POTASSIUM CHANNEL HERG; SABIPORIDE; SODIUM CHANNEL BLOCKING AGENT; SODIUM PROTON EXCHANGE PROTEIN 1; UNCLASSIFIED DRUG; ZONIPORIDE;

ACUTE HEART INFARCTION; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CALCIUM CELL LEVEL; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CHEMICAL STRUCTURE; CONTROLLED STUDY; DOG; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; EX VIVO STUDY; HEART FAILURE; HEART MUSCLE ISCHEMIA; HEART PROTECTION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HUMAN TISSUE; ISOLATED HEART; LIVER MICROSOME; MALE; MASS SPECTROMETRY; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PROTEIN EXPRESSION; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; THROMBOCYTE;

ANIMALS; BENZAMIDES; BIOLOGICAL AVAILABILITY; BLOOD PLATELETS; CELL LINE; CELL MEMBRANE PERMEABILITY; CELL SIZE; CYTOCHROME P-450 ENZYME SYSTEM; DOGS; ETHER-A-GO-GO POTASSIUM CHANNELS; GUANIDINES; HUMANS; MALE; MEMBRANES, ARTIFICIAL; MICROSOMES, LIVER; MODELS, MOLECULAR; MYOCARDIAL INFARCTION; MYOCARDIAL REPERFUSION INJURY; PERMEABILITY; PROTEIN ISOFORMS; RATS; RATS, SPRAGUE-DAWLEY; SODIUM-HYDROGEN ANTIPORTER; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84866910244     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300601d     Document Type: Article

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