Imaging and Quantitation of Cannabinoid CB₁ Receptors in Human and Monkey Brains Using ¹⁸F-Labeled Inverse Agonist Radioligands

Abstract

Studies in monkeys facilitated our development and selection of (18)F-FMPEP-d(2), compared with (18)F-FMPEP, as a radioligand demonstrating high brain uptake, high percentage of specific binding, and reduced uptake in bone. Retest analysis in human subjects showed that (18)F-FMPEP-d(2) has greater precision and accuracy than (11)C-MePPEP, allowing smaller sample sizes to detect a significant difference between groups.