title: Targeted zwitterionic near infrared fluorescent probe for improved imaging of type 2 cannabinoid receptors.
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.
authors.affiliation: University of Pittsburgh, Department of Radiology, Molecular Imaging Laboratory, Pittsburgh, Pennsylvania 15219bShanghai Jiao Tong University, School of Medicine, Ruijin Hospital, Department of Radiology, Shanghai 200025, China.
authors.forename: Zhiyuan
authors.initials: Z
authors.lastname: Wu
authors.affiliation: University of Pittsburgh, Department of Radiology, Molecular Imaging Laboratory, Pittsburgh, Pennsylvania 15219.
authors.forename: Pin
authors.initials: P
authors.lastname: Shao
authors.affiliation: University of Pittsburgh, Department of Radiology, Molecular Imaging Laboratory, Pittsburgh, Pennsylvania 15219cXi'an Jiaotong University, the First Hospital of Medical School, Department of Diagnostic Radiology, Xi'an, Shaanxi 710061, China.
authors.forename: Shaojuan
authors.initials: S
authors.lastname: Zhang
authors.affiliation: University of Pittsburgh, Department of Radiology, Molecular Imaging Laboratory, Pittsburgh, Pennsylvania 15219dUniversity of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania 15232.
authors.forename: Mingfeng
authors.initials: M
authors.lastname: Bai
mesh_terms: D000818:Animals; D001952:Bridged-Ring Compounds / Q000737:chemistry / Q000378:metabolism*; D045744:Cell Line, Tumor; D005260:Female; D005456:Fluorescent Dyes / Q000737:chemistry / Q000378:metabolism*; D051379:Mice; D008819:Mice, Nude; D015335:Molecular Probes / Q000737:chemistry / Q000378:metabolism*; D061848:Optical Imaging / Q000379:methods*; D011720:Pyrazoles / Q000737:chemistry / Q000378:metabolism*; D043885:Receptor, Cannabinoid, CB2 / Q000032:analysis* / Q000737:chemistry / Q000378:metabolism*
chemical_list: D001952:Bridged-Ring Compounds; D005456:Fluorescent Dyes; C532005:MBC94; D015335:Molecular Probes; D011720:Pyrazoles; D043885:Receptor, Cannabinoid, CB2