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Isozyme-nonselective N-Substituted Bipiperidylcarboxamide Acetyl-CoA Carboxylase Inhibitors Reduce Tissue Malonyl-CoA Concentrations, Inhibit Fatty Acid Synthesis, and Increase Fatty Acid Oxidation
TLDR
Observed properties of CP-610431 and CP-640186 indicate that isozyme-nonselective ACC inhibition has the potential to favorably affect risk factors associated with the metabolic syndrome. Expand
Expression of multiple isoforms of nitric oxide synthase in normal and atherosclerotic vessels.
TLDR
There is a loss of ecNOS expression by endothelial cells over advanced atherosclerotic lesions and a significant increase in overall NOS synthesis by other cell types in advanced lesions composed of the ecN OS, nNOS, and iNOS isoforms. Expand
Differing cardioprotective efficacy of the Na+/Ca2+ exchanger inhibitors SEA0400 and KB-R7943.
TLDR
The ability of KB-R7943 to provide cardioprotection is modest and limited by negative effects on cardiac function, whereas the more selective NCX inhibitor SEA0400 elicits marked reductions in myocardial ischemic injury and improved +/-dP/dt. Expand
In vivo pharmacological evaluation of two novel type II (inducible) nitric oxide synthase inhibitors.
TLDR
Although EIT and AMT are potent inhibitors of type II NOS function in vivo, type IINOS inhibitors of even greater selectivity may need to be developed for therapeutic applications, including treatment of sepsis, diabetes, and autoimmune diseases. Expand
Lipopolysaccharide-induced changes in plasma nitrite and nitrate concentrations in rats and mice: pharmacological evaluation of nitric oxide synthase inhibitors.
TLDR
Models provide a simple and reproducible means for assessing the in vivo inhibition of type II NOS by various compounds and suggest inhibition of the type I (neuronal) or type III (endothelial) NOS, rather than the type II isoform, may be a possible mechanism for animal mortality. Expand
Selective activation of adenosine A3 receptors with N6-(3-chlorobenzyl)-5'-N-methylcarboxamidoadenosine (CB-MECA) provides cardioprotection via KATP channel activation.
TLDR
CB-MECA is a novel 100-fold A3 receptor-selective agonist which should prove useful for elucidating A3-dependent mechanisms in the rabbit heart. Expand
Isoforms of nitric oxide synthase: functions in the cardiovascular system.
TLDR
Endothelium-derived NO is a physiologically significant vasodilator and inhibitor of platelet aggregation and adhesion, and vascular NO can prevent leukocyte adhesion to the endothelium by interfering with the adhesion molecule CD11/CD18, and NO has also been shown to inhibit the proliferation of vascular smooth muscle cells. Expand
Zoniporide: a potent and highly selective inhibitor of human Na(+)/H(+) exchanger-1.
TLDR
It is concluded that zoniporide represents a novel, potent and highly selective NHE-1 inhibitor. Expand
Selective adenosine A3 receptor stimulation reduces ischemic myocardial injury in the rabbit heart.
TLDR
These data clearly demonstrate that selective A3 receptor activation provides cardioprotection from ischemia-reperfusion injury in the rabbit heart and the degree of A3-dependent cardioprotsection is similar to that provided by A1 receptor stimulation or ischemic preconditioning. Expand
A novel sodium-hydrogen exchanger isoform-1 inhibitor, zoniporide, reduces ischemic myocardial injury in vitro and in vivo.
TLDR
Zoniporide represents a novel class of potent NHE-1 inhibitors with potential utility for providing clinical cardioprotection and did not cause any in vivo hemodynamic changes. Expand
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