Exploring occupancy of the histamine H₃ receptor by pitolisant in humans using PET.

ABSTRACT:

Background and purpose

BF2.649 (pitolisant, Wakix®) is a novel histamine H₃ receptor inverse agonist/antagonist recently approved for the treatment of narcolepsy disorder. The objective of the study was to investigate in vivo occupancy of H₃ receptors by BF2.649 using PET brain imaging with the H₃ receptor antagonist radioligand [¹¹ C]GSK189254.

Experimental approach

Six healthy adult participants were scanned with [¹¹ C]GSK189254. Participants underwent a total of two PET scans on separate days, 3 h after oral administration of placebo or after pitolisant hydrochloride (40 mg). [¹¹ C]GSK189254 regional total distribution volumes were estimated in nine brain regions of interest with the two tissue-compartment

SUBMITTER: Rusjan P 

PROVIDER: S-EPMC7348085 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature