—1. The effect of pentamethylene tetrazole (PTZ) or metrazol on rat brain phosphorylase (E.C.220.127.116.11.) was studied in vitro. The inhibitory action of PTZ was dependent on its concentration, being most marked in about 4 mM concentration. The inhibitory effect could be reversed to a great extent by inclusion of 5’AMP in the preincubation mixture. GMP, UMP and pyridoxal phosphate had no protective action under similar conditions.
2. PTZ did not appear to be a general inhibitor of enzymes. It had no effect on the activity of rat brain guanine deaminase, E. coli RNA-polymerase, or E. coli aspartate kinase. The inhibition of rat liver phosphorylase activity by PTZ was of a lower order (20 per cent) in comparison with that of brain phosphorylase (56 per cent).
3. Megimide, another convulsant drug, also inhibited the brain phosphorylase in vitro, but the effect of Nikethamide was not so pronounced. Pentothal sodium (a sedative drug) had very little effect on the brain phosphorylase activity.