Literature DB >> 18042383

Design and synthesis of a fluorescent muscarinic antagonist.

Lyn H Jones1, Amy Randall, Carolyn Napier, Mike Trevethick, Sasha Sreckovic, Jessica Watson.   

Abstract

The design and concise synthesis of a fluorescent tolterodine-BODIPY (boron dipyrromethene) conjugate is described which possesses potent antimuscarinic activity. This derivative illustrates proof-of-concept for the preparation of other useful fluorophoric antimuscarinic agents which have potential utility in receptor occupancy studies and high throughput screens.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 18042383     DOI: 10.1016/j.bmcl.2007.11.022

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


  3 in total

Review 1.  The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs.

Authors:  Andrea J Vernall; Stephen J Hill; Barrie Kellam
Journal:  Br J Pharmacol       Date:  2014-03       Impact factor: 8.739

2.  Microscopic binding of M5 muscarinic acetylcholine receptor with antagonists by homology modeling, molecular docking, and molecular dynamics simulation.

Authors:  Xiaoqin Huang; Guangrong Zheng; Chang-Guo Zhan
Journal:  J Phys Chem B       Date:  2011-12-20       Impact factor: 2.991

3.  Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M2R affinity.

Authors:  Corinna G Gruber; Andrea Pegoli; Christoph Müller; Lukas Grätz; Xueke She; Max Keller
Journal:  RSC Med Chem       Date:  2020-06-08
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.