Targeted zwitterionic near infrared fluorescent probe for improved imaging of type 2 cannabinoid receptors

J Biomed Opt. 2014 Mar;19(3):36006. doi: 10.1117/1.JBO.19.3.036006.

Abstract

Recent studies indicate that the type 2 cannabinoid receptors (CB2R) have become an attractive target for treating a variety of pathologies, including cancers, neurodegenerative diseases, inflammation, pain, osteoporosis, immunological disorders and drug abuse. In addition, it appears that many of these diseases have up-regulated CB2R expression. However, the precise role of CB2R in the regulation of diseases remains unclear. The ability to specifically image CB2R would contribute to develop reliable CB2R-based therapeutic approaches with a better understanding of the mechanism of CB2R action in these diseases. We developed a CB2R-targeted zwitterionic near-infrared (NIR) fluorescent probe, ZW760-mbc94. When compared with a previously reported CB2R probe (NIR760-mbc94) with the same targeting moiety but a charged NIR fluorescent dye, ZW760-mbc94 showed improved binding specificity in vitro and ex vivo. Overall, ZW760-mbc94 appears to have great potential as a CB2R-targeted contrast agent.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Bridged-Ring Compounds / chemistry
  • Bridged-Ring Compounds / metabolism*
  • Cell Line, Tumor
  • Female
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / metabolism*
  • Mice
  • Mice, Nude
  • Molecular Probes / chemistry
  • Molecular Probes / metabolism*
  • Optical Imaging / methods*
  • Pyrazoles / chemistry
  • Pyrazoles / metabolism*
  • Receptor, Cannabinoid, CB2 / analysis*
  • Receptor, Cannabinoid, CB2 / chemistry
  • Receptor, Cannabinoid, CB2 / metabolism*

Substances

  • Bridged-Ring Compounds
  • Fluorescent Dyes
  • MBC94
  • Molecular Probes
  • Pyrazoles
  • Receptor, Cannabinoid, CB2