We recently reported that nitric oxide synthase in the brain can be inhibit
ed not only by nitro-L-arginine (L-NA) but also by its D-enantiomer nitro-D
-arginine (D-NA). In the present study, we found that D-NA, when tested in
vitro, was 400 times less potent than L-NA. However, when D-NA was injected
in vivo, its L-enantiomer, L-NA, was found to rapidly appear in plasma sam
ples (similar to 1 min), rose to a maximum concentration at 30 min (similar
to 40% conversion), and remained at this plateau for about 5 h. This was c
onsistent with the changes in blood pressure. There was no conversion of L-
to D-NA. The results suggested that D-NA has very weak biological actions
by itself, but when administered in vivo, D-NA can be converted to L-NA.