Abstract
This review includes the non-patent literature up to October 2004 that deals with selective neuronal nitric oxide synthase inhibitors (highest potency is for the neuronal isozyme). Some non-selective inhibitors or selective inducible nitric oxide synthase inhibitors are mentioned if they are related to compounds that are discussed; structures of these compounds generally are not given. In vitro inhibition constants are given either as IC50 values or as Ki values. An IC50 value, the inhibitor concentration that produces 50% inhibition in the presence of a constant concentration of substrate, is obtained by extrapolation of several rate data points to 50% inhibition. Ki values are derived from several types of plots that relate the concentration of inhibitor with enzyme velocity in the presence of a variety of substrate concentrations [1]. The Ki value can be estimated from the IC50 value [2]. Although the two inhibition constants are related, they are not the same; generally, the reported Ki values tend to be lower than the IC50 values. If specifics are desired about how the data were collected, then the reader will have to look in the literature cited. No attempt was made to be exhaustive in citing all references related to specific inhibitors; rather, examples of literature references are given for each inhibitor described.
Keywords: cell-signaling agent, l-arginine, endothelial cells, macrophage, nos isoforms, protein-protein interactions, guanidine, isothioureidos, tetrahydrobiopterin, calmodulin
Current Topics in Medicinal Chemistry
Title: Selective Neuronal Nitric Oxide Synthase Inhibitors
Volume: 5 Issue: 7
Author(s): Erik P. Erdal, Elizabeth A. Litzinger, Jiwon Seo, Yaoqiu Zhu, Haitao Ji and Richard B. Silverman
Affiliation:
Keywords: cell-signaling agent, l-arginine, endothelial cells, macrophage, nos isoforms, protein-protein interactions, guanidine, isothioureidos, tetrahydrobiopterin, calmodulin
Abstract: This review includes the non-patent literature up to October 2004 that deals with selective neuronal nitric oxide synthase inhibitors (highest potency is for the neuronal isozyme). Some non-selective inhibitors or selective inducible nitric oxide synthase inhibitors are mentioned if they are related to compounds that are discussed; structures of these compounds generally are not given. In vitro inhibition constants are given either as IC50 values or as Ki values. An IC50 value, the inhibitor concentration that produces 50% inhibition in the presence of a constant concentration of substrate, is obtained by extrapolation of several rate data points to 50% inhibition. Ki values are derived from several types of plots that relate the concentration of inhibitor with enzyme velocity in the presence of a variety of substrate concentrations [1]. The Ki value can be estimated from the IC50 value [2]. Although the two inhibition constants are related, they are not the same; generally, the reported Ki values tend to be lower than the IC50 values. If specifics are desired about how the data were collected, then the reader will have to look in the literature cited. No attempt was made to be exhaustive in citing all references related to specific inhibitors; rather, examples of literature references are given for each inhibitor described.
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Erdal P. Erik, Litzinger A. Elizabeth, Seo Jiwon, Zhu Yaoqiu, Ji Haitao and Silverman B. Richard, Selective Neuronal Nitric Oxide Synthase Inhibitors, Current Topics in Medicinal Chemistry 2005; 5 (7) . https://dx.doi.org/10.2174/1568026054679317
DOI https://dx.doi.org/10.2174/1568026054679317 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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