Synthesis of [82Br]bromperidol and preliminary tissue distribution studies in the rat

Publisher Website
Google Scholar
Abstract
A procedure is described for the preparation of the neuroleptic [82Br]bromperidol with specific activity 440 .mu.Ci/mg. The incorporation of 82Br into the molecule was accomplished through Brackman and Smit''s modification of the Sandmeyer reaction, during the last step of the synthetic route. This involved the formation of a complex between Cu82Br2 and nitric oxide gas in acetonitrile, which was then allowed to react with 4-[4-(aminophenyl)-4-hydroxy-piperidinyl]-1-(4-fluorophenyl)-1-butanone (aminoperidol) to give [82Br]bromperidol in about 1.5 h. Cupric [82Br]bromide was prepared in situ from K82Br and CuSO4.cntdot.5H2O. The radiochemical and chemical yields for the preparation of [82Br]bromperidol from K82Br were 10.4 and 12%, respectively. Preliminary tissue distribution studies with the labeled bromperidol in the rat showed that the uptake of radioactivity by the liver, brain, kidneys and the lungs was very fast and was in the declining phase in the latter 3 organs 15 min after i.v. administration.

This publication has 2 references indexed in Scilit: