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

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Abstract

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.

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Journal

Journal ID (iso-abbrev): Br J Pharmacol

Title: British journal of pharmacology

Publisher: Wiley

ISSN (Electronic): 1476-5381

ISSN (Print): 0007-1188

Publication date (Electronic): August 2020

Volume: 177

Issue: 15

Affiliations

[1 ] Research Imaging Centre, CAMH, Toronto, Canada.

[2 ] Department of Pharmacology and Toxicology, University of Toronto, Toronto, Canada.

[3 ] Campbell Family Mental Health Research Institute, CAMH, Toronto, Canada.

[4 ] Translational Addiction Research Laboratory, CAMH, Toronto, Canada.

[5 ] Institute for Mental Health Policy Research, CAMH, Toronto, Canada.

[6 ] Institute of Medical Sciences, University of Toronto, Toronto, Canada.

[7 ] Division of Brain and Therapeutics, Department of Psychiatry, University of Toronto, Toronto, Canada.

[8 ] Bioprojet Pharma, Paris, France.

[9 ] Bioprojet Biotech, Paris, France.

[10 ] Acute Care Program, CAMH, Toronto, Canada.

[11 ] Department of Family and Community Medicine, University of Toronto, Toronto, Canada.

Article

DOI: 10.1111/bph.15067

PMC ID: 7348085

PubMed ID: 32293706

SO-VID: 21aeaf82-0daf-4cd6-a1b3-a9242c9cfed0

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