Characterising the plasma-target occupancy relationship of the neurokinin antagonist GSK1144814 with PET

GSK1144814 is a potent, insurmountable antagonist at human NK1 and NK3 receptors. Understanding the relationship between plasma pharmacokinetics and receptor occupancy in the human brain, was crucial for dose selection in future clinical studies. GSK1144814 occupancy data were acquired in parallel w...

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Veröffentlicht in:	Journal of psychopharmacology (Oxford) 2014-03, Vol.28 (3), p.244-253
Hauptverfasser:	Ridler, Khanum, Gunn, Roger N, Searle, Graham E, Barletta, Julien, Passchier, Jan, Dixson, Luanna, Hallett, William A, Ashworth, Sharon, Gray, Frank A, Burgess, Clare, Poggesi, Italo, Bullman, Jonathan N, Ratti, Emiliangelo, Laruelle, Marc A, Rabiner, Eugenii A
Format:	Artikel
Sprache:	eng
Schlagworte:	Adult Biological and medical sciences Brain Brain - diagnostic imaging Brain - drug effects Brain - metabolism Clinical trials Humans Light Male Medical sciences Middle Aged Neurokinin-1 Receptor Antagonists - pharmacokinetics Neuropharmacology Pharmacology. Drug treatments Plasma Radionuclide Imaging Receptors, Neurokinin-1 - metabolism
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