MBC94, a conjugable ligand for cannabinoid CB 2 receptor imaging.

Bai M, Sexton M, Stella N, Bornhop DJ
Bioconjug Chem. 2008 19 (5): 988-92

PMID: 18444670 · PMCID: PMC4180707 · DOI:10.1021/bc700419e

Cannabinoid CB 2 receptor is a particularly attractive target for noninvasive imaging of neuroinflammation and monitoring of therapeutic efficacy. Its expression is low to undetectable in healthy brain and induced in resident microglial cells (the macrophage of the brain) after cerebral ischemia, injury, and in neuroinflammatory disease. Additionally, immune cells migrating across the blood-brain barrier typically express CB 2 receptors, which adds to the expression pool of this target and provides a reliable indicator of inflammation in the brain. Here, we synthesized a novel conjugable CB 2 receptor ligand, mbc94, which has a terminal amino group that allows for facile conjugation to imaging moieties. A near-infrared (NIR) dye labeled mbc94, NIRmbc94, was developed for CB 2 targeted imaging. Preliminary evidence, including in vitro fluorescence imaging and a competition study, showed that NIRmbc94 specifically labeled CB 2-expressing cells.

MeSH Terms (20)

Animals Astrocytoma Binding, Competitive Bridged-Ring Compounds Camphanes Cell Line, Tumor Diagnostic Imaging Dose-Response Relationship, Drug Fluorescent Dyes Ligands Mice Microscopy, Fluorescence Molecular Structure Pyrazoles Receptor, Cannabinoid, CB2 Sensitivity and Specificity Spectrometry, Fluorescence Spectroscopy, Near-Infrared Stereoisomerism Structure-Activity Relationship

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