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

Bioconjugate Chemistry
Mingfeng BaiDarryl J Bornhop

Abstract

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.

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Citations

Dec 17, 2008·Pharmaceutical Research·Esmaiel Jabbari
Oct 30, 2009·Bioconjugate Chemistry·Lynn E SamuelsonDarryl J Bornhop
Jun 17, 2011·Journal of Medicinal Chemistry·Lidia Martín-CouceSilvia Ortega-Gutiérrez
Sep 11, 2010·Chemical Communications : Chem Comm·Animesh SamantaYoung-Tae Chang
Jul 2, 2014·Journal of Medicinal Chemistry·Zhao MaMinyong Li
Sep 24, 2013·Biochimica Et Biophysica Acta·Rajashri SridharanMark E Dumont
Jun 13, 2012·Angewandte Chemie·Lidia Martín-CouceSilvia Ortega-Gutiérrez
Jun 29, 2017·Pharmacological Reviews·Anna CooperAndrea J Vernall
Nov 27, 2009·Expert Opinion on Therapeutic Patents·Ganesh A ThakurAlexandros Makriyannis
Jun 6, 2013·British Journal of Pharmacology·Andrea J VernallBarrie Kellam
Mar 19, 2021·Chemistry : a European Journal·Carlotta BorgarelliErmal Ismalaj
Sep 10, 2020·Journal of the American Chemical Society·Roman C SarottErick M Carreira

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