Quantification of [¹¹C]Ro15-4513 GABA_Aα5 specific binding and regional selectivity in humans.

ABSTRACT: [¹¹C]Ro15-4513 has been introduced as a positron emission tomography radioligand to image the GABA_Aα5 receptor subtype thought to be important in learning, memory and addiction. However, the in vivo selectivity of the ligand remains unknown and a full assessment of different analysis approaches has yet to be performed. Using human heterologous competition data, with [¹¹C]Ro15-4513 and the highly selective GABA_Aα5 selective negative allosteric modulator Basmisanil (RG1662), we quantify the GABA_Aα5 selectivity of [¹¹C]Ro15-4513, assess the validity of reference tissues and evaluate the performance of four different kinetic analysis methods. The results show that [¹¹C]Ro15-4513 has high but not complete selectivity f

SUBMITTER: Myers JF 

PROVIDER: S-EPMC5464707 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature