Literature DB >> 15993070

Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.

Andrew S Yates1, Stephen W Doughty, David A Kendall, Barrie Kellam.   

Abstract

In silico modelling was used to guide the positioning of the fluorescent dye NBD-F on the cannabinoid CB2 receptor agonist JWH-015. While the ultimate fluorescent conjugate lost extensive binding affinity to the cannabinoid CB2 receptor, affinity and efficacy studies on the naphthoyl 3-position modified precursor molecules have provided new insight into structure-activity relationships associated with this position.

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Year:  2005        PMID： 15993070     DOI： 10.1016/j.bmcl.2005.05.049

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

Review 1.  Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 selective ligands.

Authors:  A Poso; J W Huffman
Journal:  Br J Pharmacol       Date:  2007-11-05       Impact factor: 8.739

Review 2.  Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.

Authors:  Rajashri Sridharan; Jeffrey Zuber; Sara M Connelly; Elizabeth Mathew; Mark E Dumont
Journal:  Biochim Biophys Acta       Date:  2013-09-18

3.  Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells.

Authors:  Ravil R Petrov; Maria E Ferrini; Zeina Jaffar; Charles M Thompson; Kevan Roberts; Philippe Diaz
Journal:  Bioorg Med Chem Lett       Date:  2011-08-03       Impact factor: 2.823

4.  Mutagenesis and computer modeling studies of a GPCR conserved residue W5.43(194) in ligand recognition and signal transduction for CB2 receptor.

Authors:  Yuxun Zhang; Zhaojun Xie; Lirong Wang; Brielle Schreiter; John S Lazo; Jurg Gertsch; Xiang-Qun Xie
Journal:  Int Immunopharmacol       Date:  2011-05-01       Impact factor: 4.932

5.  In vivo inflammation imaging using a CB2R-targeted near infrared fluorescent probe.

Authors:  Shaojuan Zhang; Pin Shao; Xiaoxi Ling; Ling Yang; Weizhou Hou; Steve H Thorne; Wissam Beaino; Carolyn J Anderson; Ying Ding; Mingfeng Bai
Journal:  Am J Nucl Med Mol Imaging       Date:  2015-02-15

6.  A novel near-infrared fluorescence imaging probe that preferentially binds to cannabinoid receptors CB2R over CB1R.

Authors:  Xiaoxi Ling; Shaojuan Zhang; Pin Shao; Weixia Li; Ling Yang; Ying Ding; Cong Xu; Nephi Stella; Mingfeng Bai
Journal:  Biomaterials       Date:  2015-04-28       Impact factor: 12.479

7.  Theoretical study of the regioselective cyclization of enaminones in the construction of benzofurans and indoles.

Authors:  Rafael Herrera; Francisco Méndez; Fabiola Jiménez; M Carmen Cruz; Joaquín Tamariz
Journal:  J Mol Model       Date:  2016-04-30       Impact factor: 1.810

8.  Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells.

Authors:  Marjolein Soethoudt; Sara C Stolze; Matthias V Westphal; Luuk van Stralen; Andrea Martella; Eva J van Rooden; Wolfgang Guba; Zoltan V Varga; Hui Deng; Sander I van Kasteren; Uwe Grether; Adriaan P IJzerman; Pal Pacher; Erick M Carreira; Herman S Overkleeft; Andreea Ioan-Facsinay; Laura H Heitman; Mario van der Stelt
Journal:  J Am Chem Soc       Date:  2018-02-16       Impact factor: 15.419

Review 9.  Functionalized Cannabinoid Subtype 2 Receptor Ligands: Fluorescent, PET, Photochromic and Covalent Molecular Probes.

Authors:  Filippo Basagni; Michela Rosini; Michael Decker
Journal:  ChemMedChem       Date:  2020-06-24       Impact factor: 3.466
  9 in total

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