TABLE 2

NOS inhibition vs. inhibition of glufosinate-induced convulsions

NOS inhibition in the cerebellum was monitored by NOS assay in vivo. NOS inhibition is presented as the percentage of inhibition compared with each vehicle treatment. Vehicle was peanut oil for the indazole analogs and physiological saline for the imidazole and arginine analogs. Results are given as means ± S.E. (n = 3 or 4). Citrulline productions with each vehicle treatment, normalized as 100% to calculate the percentage of inhibition values of NOS inhibition, were 29.0 ± 2.6 (a), 29.8 ± 1.6 (b), 34.0 ± 0.9 (c), and 31.5 ± 1.5 (d) (picomoles per milligram of protein per 15 min; n = 3 or 4). The incidences of convulsions with 7-NI, 6-NI, indazole, and vehicle (peanut oil) at 360 min after glufosinate injection (see Fig. 3) were 26.6, 20.0, 33.3, and 58.8%, respectively; these values were used for the percentage of inhibition calculations shown in the table. The incidences of convulsions with l-NAME and vehicle (saline) at 360 min after glufosinate injection (see Fig. 2A) were equal (53.3%), such that the percentage of inhibition was 0%, as shown in the table. The incidences of convulsions with l-NIO and vehicle (saline) at 360 min after glufosinate injection (see Fig. 2B) were 73.3 and 56.3%, such that the percentage of inhibition was –30%, as shown in the table.


Compound

Structure

NOS Inhibition

Anticonvulsant Activity
% inhibition
Indazole analog
7-NI Embedded Image 85.8 ± 0.9* (a) 55
6-NI Embedded Image 15.3 ± 7.3 (a) 66
Indazole Embedded Image 11.9 ± 8.3 (a) 43
Imidazole analog
TRIM Embedded Image 39.7 ± 2.3 (b) 100
Arginine analog
l-NAME Embedded Image 93.0 ± 0.7* (c) 0
l-NIO
Embedded Image
80.7 ± 1.2* (d)
-30
  • * P < 0.01, Student's t test.