Agmatine, decarboxylated arginine, is a metabolic product of mammalian cells. Considering the close structural similarity between L-arginine and agmatine, we investigated the interaction of agmatine and nitric oxide synthases (NOSs), which use L-arginine to generate nitric oxide (NO) and citrulline. Brain, macrophages and endothelial cells were respectively used as sources for NOS isoforms I, II and III. Enzyme activity was measured by the production of nitrites or L-citrulline. Agmatine was a competitive NOS inhibitor but not an NO precursor. Ki values were approx. 660 μM (NOS I), 220 μM (NOS II) and 7.5 mM (NOS III). Structurally related polyamines did not inhibit NOS activity. Agmatine, therefore, may be an endogenous regulator of NO production in mammals.
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Research Article|
May 15 1996
Inhibition of mammalian nitric oxide synthases by agmatine, an endogenous polyamine formed by decarboxylation of arginine
Elena GALEA;
Elena GALEA
*
1Division of Neurobiology, Department of Neurology and Neuroscience, Cornell University Medical College, 411 East 69th Street, New York, NY 10021, U.S.A.
*To whom correspondence should be addressed.
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S. REGUNATHAN;
S. REGUNATHAN
1Division of Neurobiology, Department of Neurology and Neuroscience, Cornell University Medical College, 411 East 69th Street, New York, NY 10021, U.S.A.
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Vassily ELIOPOULOS;
Vassily ELIOPOULOS
1Division of Neurobiology, Department of Neurology and Neuroscience, Cornell University Medical College, 411 East 69th Street, New York, NY 10021, U.S.A.
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Douglas L. FEINSTEIN;
Douglas L. FEINSTEIN
1Division of Neurobiology, Department of Neurology and Neuroscience, Cornell University Medical College, 411 East 69th Street, New York, NY 10021, U.S.A.
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Donald J. REIS
Donald J. REIS
1Division of Neurobiology, Department of Neurology and Neuroscience, Cornell University Medical College, 411 East 69th Street, New York, NY 10021, U.S.A.
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Publisher: Portland Press Ltd
Received:
September 22 1995
Revision Received:
October 26 1995
Accepted:
November 08 1995
Online ISSN: 1470-8728
Print ISSN: 0264-6021
The Biochemical Society, London © 1996
1996
Biochem J (1996) 316 (1): 247–249.
Article history
Received:
September 22 1995
Revision Received:
October 26 1995
Accepted:
November 08 1995
Citation
Elena GALEA, S. REGUNATHAN, Vassily ELIOPOULOS, Douglas L. FEINSTEIN, Donald J. REIS; Inhibition of mammalian nitric oxide synthases by agmatine, an endogenous polyamine formed by decarboxylation of arginine. Biochem J 15 May 1996; 316 (1): 247–249. doi: https://doi.org/10.1042/bj3160247
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