1967 Volume 16 Issue 6 Pages 251-255
Wilzbach exposure, platinum-catalyzed exposure and chemical reduction methods were applied for tritium labeling of a new local anesthetic 2-methyl-2-n-propylaminopropion-o-toluide hydrochloride (LA-012) . The highest specific activity of 1.65 mCi/mg was obtained by catalytic hydrogenation of brominated product of LA-012, which was prepared by direct bromination of LA-012. A commercial local anesthetic prilocaine could be also labeled with tritium by catalytic hydrogenation of brominated product of prilocaine like LA-012, and high specific activity of 1.5 mCi/mg was obtained. However, lidocaine did not give any brominated product available for catalytic hydrogenation. 3H-Lidocaine with a specific activity of 0.84 mCi/mg was prepared from 3H-xylidine, which was obtained by catalytic hydrogenation of 4-bromoxylidine with tritium.
