L-thiocitrulline, Dihydrochloride is a potent stereospecific inhibitor of all three isoforms of rat NOS (NOS1, NOS2, and NOS3) that has greater inhibitory activity on NOS1 (nNOS) (Ki = 60 nM) compared to NOS2 (iNOS) (Ki = 3.6 μM). L-thiocitrulline inhibition is competitive with respect to L-Arginine, a native substrate, which suggests that L-thiocitrulline preferentially occupies the L-Arginine binding site.
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