Imaging CXCR4 Expression with Iodinated and Brominated Cyclam Derivatives

ConclusionsImaging CXCR4 expression with halogenated cyclam derivatives was successful in s.c. located tumors, but not in CNS located tumors. This was largely due to the following: (i) the hydrophilicity of the radiolabeled analogues —as reflected in the “measured” radiotracer distribution (LogD) in octanol/PBS—which stands in contrast to the structure-based estimate of LogP, which was the rationale for initiating the study and (ii) the presence of a modest BTB in intracranial U87-CXCR4 gliomas and an intact BBB/BTB in t he intracranial PCNSL animal model.
Source: Molecular Imaging and Biology - Category: Molecular Biology Source Type: research