Unexpectedly high affinity of a novel histamine H3 receptor antagonist, GSK239512, in vivo in human brain, determined using PET

British Journal of Pharmacology

Volumn 171, Issue 5, 2014, Pages 1241-1249

  Ashworth, S ^a   Berges, A ^a   Rabiner, E A ^a,b   Wilson, A A ^c   Comley, R A ^a   Lai, R Y K ^a   Boardley, R ^a   Searle, G ^a   Gunn, R N ^a,b   Laruelle, M ^a,b   Cunningham, V J ^a,b,d  

^a GLAXOSMITHKLINE   (United Kingdom)

^b IMPERIAL COLLEGE LONDON   (United Kingdom)

^c CENTRE FOR ADDICTION AND MENTAL HEALTH   (Canada)

^d UNIVERSITY OF ABERDEEN   (United Kingdom)

Author keywords

drug development; PET study; pharmacokinetics; receptor occupancy

Indexed keywords

GSK 239512; HISTAMINE H3 RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

AMYGDALOID NUCLEUS; ANTERIOR CINGULATE; ARTICLE; CAUDATE NUCLEUS; CEREBELLUM; DRUG BLOOD LEVEL; FRONTAL CORTEX; HIPPOCAMPUS; HUMAN; IN VIVO STUDY; INSULA; MOTOR CORTEX; NORMAL HUMAN; OCCIPITAL CORTEX; PARIETAL CORTEX; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PUTAMEN; RECEPTOR AFFINITY; THALAMUS; TIME TO MAXIMUM PLASMA CONCENTRATION;

DRUG DEVELOPMENT; H3 RECEPTORS; PET STUDY; PHARMACOKINETICS; RECEPTOR OCCUPANCY;

ADULT; BENZAZEPINES; BRAIN; HISTAMINE ANTAGONISTS; HUMANS; MALE; MIDDLE AGED; NIACINAMIDE; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RECEPTORS, HISTAMINE H3;

EID: 84895165092     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.12505     Document Type: Article

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