Search Results - "PETTERSEN, JOHN C."
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Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2)
Published in Journal of medicinal chemistry (24-09-2015)“…The medicinal chemistry and preclinical biology of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2) is described. A screening hit 1…”
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2
Discovery of a Clinical Candidate from the Structurally Unique Dioxa-bicyclo[3.2.1]octane Class of Sodium-Dependent Glucose Cotransporter 2 Inhibitors
Published in Journal of medicinal chemistry (28-04-2011)“…Compound 4 (PF-04971729) belongs to a new class of potent and selective sodium-dependent glucose cotransporter 2 inhibitors incorporating a unique…”
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3
Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis
Published in Journal of medicinal chemistry (24-11-2022)“…Discovery efforts leading to the identification of ervogastat (PF-06865571), a systemically acting diacylglycerol acyltransferase (DGAT2) inhibitor that has…”
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4
Harmonized 3Rs-based non-mutagenic impurity qualification study designs developed using the results of an IQ consortium survey
Published in Regulatory toxicology and pharmacology (01-06-2021)“…As per the ICH Q3A(R2) and Q3B(R2) regulatory guidelines, safety studies may be needed when an impurity in new drug substances or products is above the…”
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5
Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator
Published in Drug metabolism and disposition (01-11-2014)“…The present article summarizes Metabolites in Safety Testing (MIST) studies on a glucokinase activator,…”
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The PPARα Agonists Fenofibrate and CP-778875 Cause Increased β-Oxidation, Leading to Oxidative Injury in Skeletal and Cardiac Muscle in the Rat
Published in Toxicologic pathology (01-04-2012)“…Weak peroxisome proliferator–activated receptor (PPAR) α agonists (fibrates) are used to treat dyslipidemia. This study compared the effects of the potent and…”
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The Relationship of Glucokinase Activator–induced Hypoglycemia with Arteriopathy, Neuronal Necrosis, and Peripheral Neuropathy in Nonclinical Studies
Published in Toxicologic pathology (01-06-2014)“…Glucokinase activators (GKAs) are being developed for the treatment of type 2 diabetes. The toxicity of 4 GKAs (PF-04279405, PF-04651887, piragliatin, and…”
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The Development of Subcutaneous Sarcomas in Rodents Exposed to Peroxisome Proliferators Agonists: Hypothetical Mechanisms of Action and De-Risking Attitude
Published in Toxicologic pathology (01-07-2012)“…Peroxisome proliferator-activated receptors (PPARs) represent therapeutic targets for the management of type 2 diabetes mellitus and dyslipidemia. Rodent…”
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Neurotoxic Effects of Zoniporide: A Selective Inhibitor of the Na+/H+ Exchanger Isoform 1
Published in Toxicologic pathology (01-06-2008)“…Zoniporide, an inhibitor of the Na+-H+ exchanger-1, was administered by continuous intravenous infusion to rats and dogs for up to 1 month. In 1-month studies,…”
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10
Discovery and biological characterization of capromorelin analogues with extended half-lives
Published in Bioorganic & medicinal chemistry letters (18-11-2002)“…New tert-butyl, picolyl and fluorinated analogues of capromorelin ( 3), a short-acting growth hormone secretagogue (GHS), were prepared as part of a program to…”
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11
The effects of cyanide on brain mitochondrial cytochrome oxidase and respiratory activities
Published in Journal of applied toxicology (01-01-1993)“…Brain mitochondrial cytochrome oxidase and respiratory activities were compared after in vivo and in vitro exposure to cyanide. For the in vivo studies, mice…”
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Neurotoxic Effects of Zoniporide: A Selective Inhibitor of the Na super(+)/H super(+) Exchanger Isoform 1
Published in Toxicologic pathology (01-06-2008)“…Zoniporide, an inhibitor of the Na super(+)-H super(+) exchanger-1, was administered by continuous intravenous infusion to rats and dogs for up to 1 month. In…”
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A 2-Year Comparison Study of Crl:CD BR and Hsd:Sprague-Dawley SD Rats
Published in Toxicological sciences (01-10-1996)“…In this 2-year study, the suitability of the Hsd:Sprague-Dawley SD (SD) as a replacement for the Crl:CD BR (CD) rat was assessed by comparing survival rates,…”
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14
Twenty-six week toxicity study with KASAL® (basic sodium aluminum phosphate) in beagle dogs
Published in Environmental geochemistry and health (01-03-1990)“…Relatively few long-term studies in laboratory animals have been reported. Because sodium aluminum phosphate formulations are potentially important sources of…”
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Antagonism of cyanide poisoning by chlorpromazine and sodium thiosulfate
Published in Toxicology and applied pharmacology (01-01-1985)“…Anti-cyanide action by sodium thiosulfate (ST) was enhanced by prior administration of chlorpromazine (CPZ). However, CPZ (alone) provided no protection…”
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A 2-Year Comparison Study of Crl:CD BR and Hsd:Sprague–Dawley SD Rats
Published in Fundamental and applied toxicology (01-10-1996)“…In this 2-year study, the suitability of the Hsd:Sprague–Dawley SD (SD) as a replacement for the Crl:CD BR (CD) rat was assessed by comparing survival rates,…”
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17
Noninvasive measurement of systemic arterial blood pressure in the conscious beagle dog
Published in Fundamental and applied toxicology (01-01-1988)“…The objectives of this study were to evaluate a technique for routine, noninvasive measurement of systemic arterial blood pressure and heart rate (HR) in…”
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