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

• Published in: Journal of psychopharmacology (Oxford) Vol. 28; no. 3; p. 244
• Main Authors: 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: Journal Article
• Language: English
• Published: United States 01.03.2014
• Subjects: Adult; Brain - diagnostic imaging; Brain - drug effects; Brain - metabolism; Humans; Male; Middle Aged; Neurokinin-1 Receptor Antagonists - pharmacokinetics; Radionuclide Imaging; Receptors, Neurokinin-1 - metabolism; Pharmacology; PET; neurokinin

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...