Imaging the 5-HT_2C receptor with PET: Evaluation of 5-HT_2C and 5-HT_2A affinity of pimavanserin in the primate brain.

ABSTRACT: Two complimentary techniques were used to estimate occupancy of pimavanserin (a selective 5-HT_2A/2C inverse agonist) to 5-HT_2A and 5-HT_2C receptors in non-human primate brains. One employed the 5-HT_2A/2C selective radioligand [¹¹C]CIMBI-36 combined with quantification of binding potentials in brain regions known to be enriched in 5-HT_2A (cortex) or 5-HT_2C (choroid plexus) receptors to estimate occupancy. Pimavanserin was 6-10 fold more potent displacing [¹¹C]CIMBI-36 from cortex (ED₅₀ = 0.007 mg/kg; EC₅₀ = 0.6 ng/ml) than from choroid plexus (ED₅₀ =0.046 mg/kg; EC₅₀ = 6.0 ng/ml). The assignment of [¹¹C]CIMBI-36 binding to 5-HT_2A and 5-HT<

SUBMITTER: Ridler K 

PROVIDER: S-EPMC11800257 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature