Positron Emission Tomography (PET) Study to Describe the Relationship Between Plasma Concentrations and Brain Gly-T1 Occupancy of GSK1018921 Over Time.

An Adaptive PET Study in Healthy Volunteers Using [11C]GSK931145 to Establish the Relationship of Glycine Transporter 1 Occupancy by GSK1018921 to Plasma Concentrations Over Time.

A PET study using [11c]GSK931145 to characterise the exposure-occupancy relationship over time for GSK1018921.

This is an open-label, adaptive-design, single-dose, non randomized PET occupancy study.The primary aim of this study is to describe the relationship between plasma concentrations and brain occupancy of GSK1018921 over time. Up to 22 healthy volunteers will be administered single doses of GSK1018921 in order to obtain 12 evaluable complete data sets of occupancy estimates.

• Inclusion criteria:

  • Healthy male subjects
  • Age: 18-55 years
  • No history of physical, neurological or mental illness

• Exclusion criteria

  • History of claustrophobia or inability to lie still in the PET camera for at least 2 hours
  • Cardiac pacemakers or metal implants in the body that contraindicate MRI scan.
  • History of regular alcohol consumption (weekly intake >21 units) within the previous six months.