Open AccessPharmacologic characterizations of a P2X7 receptor-specific radioligand, [11C]GSK1482160 for neuroinflammatory response
Author(s) -
Jiande Han,
Hui Liu,
Chunling Liu,
Hongjun Jin,
Joel S. Perlmutter,
Terrance M. Egan,
Zhude Tu
Publication year - 2017
Publication title -
nuclear medicine communications
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.489
H-Index - 73
eISSN - 1473-5628
pISSN - 0143-3636
DOI - 10.1097/mnm.0000000000000660
Subject(s) - radioligand , experimental autoimmune encephalomyelitis , neuroinflammation , spinal cord , receptor , chemistry , in vivo , medicine , endocrinology , inflammation , biology , neuroscience , microbiology and biotechnology
The P2X7 receptor (P2X7R) is a key regulatory element in the neuroinflammatory cascade that provides a promising target for imaging neuroinflammation. GSK1482160, a P2X7R modulator with nanomolar binding affinity and high selectivity, has been successfully radiolabeled and utilized for imaging P2X7 levels in a mouse model of lipopolysaccharide-induced systemic inflammation. In the current study, we further characterized its binding profile and determined whether [C]GSK1482160 can detect changes in P2X7R expression in a rodent model of multiple sclerosis.