Ontology highlight
ABSTRACT:
SUBMITTER: Jin H
PROVIDER: S-EPMC4288033 | biostudies-literature | 2014 Nov
REPOSITORIES: biostudies-literature
Jin Hongjun H Fan Jinda J Zhang Xiang X Li Junfeng J Flores Hubert P HP Perlmutter Joel S JS Parsons Stanley M SM Tu Zhude Z
MedChemComm 20141101 11
The σ<sub>1</sub> receptor is an important target for CNS disorders. We previously identified a σ<sub>1</sub> ligand TZ3108 having highly potent (<i>K</i><sub>i-σ1</sub> = 0.48 nM) and selective affinity for σ<sub>1</sub> versus σ<sub>2</sub> receptors. TZ3108 was <sup>18</sup>F-labeled with F-18 for <i>in vivo</i> evaluation. Biodistribution and blocking studies of [<sup>18</sup>F]TZ3108 in male Sprague-Dawley rats demonstrated high brain uptake, which was σ<sub>1</sub>-specific with no <i>in v ...[more]