Unexpectedly high affinity of a novel histamine<scp>H₃</scp>receptor antagonist,<scp>GSK239512</scp>,<i>in vivo</i>in human brain, determined using<scp>PET</scp>

Abstract

The affinity of GSK239512 for brain H3 receptors in humans in vivo is much higher than that expected from studies in vitro, and higher than that observed in PET studies in pigs. The study illustrates the utility of carrying out PET studies in humans early in drug development, providing accurate quantification of GSK239512 RO in vivo as a function of time and dose.