Abstract
Risperidone and lamotrigine were successfully labeled with 125I via direct electrophilic substitution reaction at 80 °C with maximum labeling yields of 89 ± 3.75 and 97.5 ± 1.0 %, respectively. Stability of 125I-risperidone was up to 6 h while that of 125I-lamotrigine was up to 24 h. Biodistribution studies showed that maximum uptakes of 125I-risperidone and 125I-lamotrigine in the brain of mice were 4.35 ± 0.17 and 2.51 ± 0.18 % of the injected activity/g tissue organ at 10 min post-injection, respectively. Both radioiodinated drugs showed higher brain uptake and stability compared to commercially available technetium-99m d,l-hexamethyl propyleneamine oxime.
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