Unexpectedly high affinity of a novel histamine H(3) receptor antagonist, GSK239512, in vivo in human brain, determined using PET.

Ashworth, S; Berges, A; Rabiner, E A; Wilson, A A; Comley, R A; Lai, R Y K; Boardley, R; Searle, G; Gunn, R N; Laruelle, M; Cunningham, V J

Ashworth, S; Berges, A; Rabiner, E A; Wilson, A A; Comley, R A; Lai, R Y K; Boardley, R; Searle, G; Gunn, R N; Laruelle, M; Cunningham, V J.

Affiliation

Ashworth S; GlaxoSmithKline Clinical Imaging Centre, London, UK.

Br J Pharmacol ; 171(5): 1241-9, 2014 Mar.

Article in En | MEDLINE | ID: mdl-24670146

Subject(s)

Benzazepines/pharmacokinetics; Brain/metabolism; Histamine Antagonists/pharmacokinetics; Niacinamide/analogs & derivatives; Receptors, Histamine H3/metabolism; Adult; Benzazepines/blood; Brain/diagnostic imaging; Histamine Antagonists/blood; Humans; Male; Middle Aged; Niacinamide/blood; Niacinamide/pharmacokinetics; Positron-Emission Tomography; Radiopharmaceuticals/blood; Radiopharmaceuticals/pharmacokinetics

Key words

H3 receptors; PET study; drug development; pharmacokinetics; receptor occupancy

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzazepines / Brain / Niacinamide / Receptors, Histamine H3 / Histamine Antagonists Limits: Adult / Humans / Male / Middle aged Language: En Journal: Br J Pharmacol Year: 2014 Document type: Article Affiliation country: United kingdom Country of publication: United kingdom

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