Frontiers in Medicinal Chemistry

Volume: 4

Indexed in: BIOSIS Previews, EMBASE, Chemical Abstracts, EBSCO, Ulrich's Periodicals Directory.

“Frontiers in Medicinal Chemistry” is an Ebook series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. “Frontiers in ...
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Selective Neuronal Nitric Oxide Synthase Inhibitors

Pp. 842-882 (41)

Haitao Ji, Erik P. Erdal, Elizabeth A. Litzinger, Jiwon Seo, Yaoqiu Zhu, Fengtian Xue, Jianguo Fang, Jinwen Huang and Richard B. Silverman


This review includes the non-patent literature up to August 2008 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.


Department of Chemistry, Department of Biochemistry, Molecular Biology, and Cell Biology, and Center for Drug Discovery and Chemical Biology, Northwestern University, Evanston, Illinois 60208-3113 USA.