Pharmacology and Clinical Pharmacology of Methylarginines Used as Inhibitors of Nitric Oxide Synthases
Anja Kittel and Renke Maas
Affiliation: Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander-Universitat Erlangen-Nurnberg, Fahrstraße 17, 91054 Erlangen, Germany.
The methylarginines asymmetric dimethylarginine (ADMA) and monomethylarginine (L-NMMA) are endogenously formed
inhibitors of nitric oxide synthases (NOS), which have extensively been investigated as risk markers and used as pharmacological tools to
study the L-arginine-nitric oxide (NO) pathway in vitro and in vivo. It is the aim of the present review to summarize the clinical and experimental
data on the pharmacological properties that are of relevance when planning and conducting experiments and clinical studies
involving methylarginines. Key pharmacodynamic and pharmacokinetic data including IC50 values of ADMA and L-NMMA for NOS
isoforms and transport proteins, as well as metabolism by dimethylarginine dimethylaminohydrolases (DDAH1 and DDAH2) and
alanine-glyoxylate aminotransferase 2 (AGXT2) are discussed.
Keywords: Asymmetric dimethylarginine (ADMA), Symmetric dimethylarginine (SDMA), Monomethylarginine (L-NMMA), Nitric oxide
synthase (NOS), Dimethylarginine dimethylaminohydrolase (DDAH), Alanine-glyoxylate aminotransferase 2 (AGXT2).
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