A potent and selective C-11 labeled PET tracer for imaging sphingosine-1-phosphate receptor 2 in the CNS demonstrates sexually dimorphic expression.

ABSTRACT: Sphingosine-1-phosphate receptor 2 (S1PR2) plays an essential role in regulating blood-brain barrier (BBB) function during demyelinating central nervous system (CNS) disease. Increased expression of S1PR2 occurs in disease-susceptible CNS regions of female versus male SJL mice and in female multiple sclerosis (MS) patients. Here we reported a novel sensitive and noninvasive method to quantitatively assess S1PR2 expression using a C-11 labeled positron emission tomography (PET) radioligand [(11)C]5a for in vivo imaging of S1PR2. Compound 5a exhibited promising binding potency with IC50 value of 9.52 ± 0.70 nM for S1PR2 and high selectivity over S1PR1 and S1PR3 (both IC50 > 1000 nM). [(11)C]5a was synthesized in ∼40 min with radiochemistry yield of 20 ± 5% (decayed to the end of bombardment

SUBMITTER: Yue X 

PROVIDER: S-EPMC4508201 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature