The purpose of this study is to investigate the relationship between the plasma concentrations of the study drug and the amount of the study drug bound to the D3 receptors of the brain after dosing of a new compound GSK618334.
This imaging study will be an open label, non-randomised PET receptor occupancy study using healthy male volunteers. The time course and degree of D3 receptor occupancy (RO) after single doses of GSK618334 will be determined using 11C-PHNO as a PET ligand labeling dopamine receptor. The PK/PD relationship between plasma concentrations of GSK618334 and D3 RO will be described. Potential relationships between D3 RO and functional magnetic resonance imaging (fMRI) endpoints will be assessed as an exploratory aim.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
12
D3 receptor antagonist
GSK Investigational Site
Harrow, Middlesex, United Kingdom
Binding of PHNO, PET ligand, in each region of interest at each scan.
Time frame: up to 48 hours
Percentage of PHNO, PET ligand, occupancy in each region of interest after a single oral dose of GSK618334 for each individual.
Time frame: up to 48 hours
Time course of GSK618334 concentration in blood following a single oral dose.
Time frame: up to 48 hours
Adverse events and other safety assessments such as clinically relevant changes in electrocardiography (ECG); vital signs (blood pressure, heart rate); laboratory safety data and physical examination.
Time frame: screening to follow-up
Measuring GSK618334 in the body (pharmacokinetic endpoints): PK parameters of GSK618334 Cmax, AUCinf, tmax.
Time frame: up to 48 hours
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