INVIVO DISTRIBUTION OF C-11 PHENYTOIN AND ITS MAJOR METABOLITE, AND THEIR USE IN SCINTIGRAPHIC IMAGING

  • 1 January 1978
    • journal article
    • research article
    • Vol. 19  (8) , 936-941
Abstract
Curie quantities (0.3-1.5 Ci) of H11CN were used in the synthesis of 11C-tagged phenytoin (C-11.DPH) and 5-(p-hydroxyphenyl)-5-phenylhydantoin (C-11.HPPH), using a modified Buecherer-Bergs reaction. The H11CN was produced from a mixture of 95% N and 5% H by a 45-min bombardment with 10-MeV protons at 10 .mu.A. Following i.v. infusions of C-11 DPH (13.7 mg/kg at a rate of 29 mg/min) into the left femoral vein of rhesus monkeys, DPH shows persistent concentration in the brain and liver fields. Extravascular administration shows significant retention at the site of administration. I.v. bolus injection of [11C]-HPPH into a rhesus monkey, at a dose of 6.4 mg/kg, resulted in localization of this compound in the liver, gallbladder, urinary bladder and intestinal fields. Loss of activity from the liver region, with appearance of this activity in the intestinal field, suggests that [11C]-HPPH was secreted into the intestine via the bile.