Dopaminergic D2 antagonist modulates expression of vesicular acetylcholine transporter in the brain of nonhuman primates.

Conclusion D2 antagonism by (-)-eticlopride at high dose (0.03 mg/kg) dramatically increased striatal uptake of [18F]VAT in NHPs, suggesting PET with [18F]VAT provides a useful tool for investigation of dopaminergic modulation on VAChT expression in the brain of living animals. The elevation of striatal [18F]VAT uptake by 0.03 mg/kg (-)-eticlopride might be attributed to the disinhibition of cholinergic transmission by D2 antagonism. Ongoing studies are exploring the impact of D2 agonism on VAChT expression in the NHP brain. These results may help guide future investigation of the effects of dopaminergic drugs on cholinergic function in humans. Research Support NS075527, NS103988. Reference 1. Tu, Z., et al. Bioorg. Med. Chem. 2015, 23, 4699-709. Figure 1. Representative PET images (top panel) and time-activity curves (lower panel) showing striatal tracer uptake of [18F]VAT was upregulated dramatically by the pretreatment with 0.03 mg/kg (-)-eticlopride.

Source: Journal of Nuclear Medicine - May 23, 2018 Category: Nuclear Medicine Authors: Liu, H., Luo, Z., Jin, H., Gu, J., Flores, H., Perlmutter, J., Tu, Z. Tags: Basic Science III Source Type: research