Presynaptic Selectivity of a Ligand for Serotonin 1A Receptors Revealed by In Vivo PET Assays of Rat Brain
Figure 2
Occupancies of 5-HT1A receptors by Wf-516 and pindolol assessed by ex vivo ARG.
(A) Representative autoradiograms showing distribution and intensity of [11C]WAY-100635 radiosignals in rat brain sections containing the hippocampus (arrows) and raphe nucleus (arrowhead) after oral administration of Wf-516 and intraperitoneal administration of pindolol. (B) Relationships between dose of Wf-516 (left) or pindolol (right) and 5-HT1A receptor occupancy in the hippocampus (closed symbols) and raphe nucleus (open symbols). Regression curves in the hippocampus and raphe nucleus are denoted by dashed lines and solid lines, respectively, and were generated by the following equation: Occ = 100×D/(D+ED50), where Occ is 5-HT1A receptor occupancy and D is the dose of the drug. Bars indicate S.E. (n = 3).