Literature DB >> 16434192

Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities.

Michael Amon1, Xavier Ligneau, Jean-Charles Schwartz, Holger Stark.   

Abstract

Omega-piperidinoalkanamine derivatives with fluorescent moieties (2-cyanoisoindol-1-yl, 7-nitrobenzofurazan-4-yl) have been synthesized starting from piperidine in three steps. The compounds display moderate to good histamine hH(3) receptor affinities with K(i) values ranging from 178 to 11nM. The new compounds may act as tools for identification and understanding of the binding site on the histamine H(3) receptor.

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Year:  2006        PMID: 16434192     DOI: 10.1016/j.bmcl.2005.12.084

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


  7 in total

Review 1.  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

2.  Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.

Authors:  Miriam Tomasch; J Stephan Schwed; Alexander Paulke; Holger Stark
Journal:  ACS Med Chem Lett       Date:  2012-12-12       Impact factor: 4.345

3.  Fluorescent Human EP3 Receptor Antagonists.

Authors:  Miriam Tomasch; J Stephan Schwed; Karina Kuczka; Sascha Meyer Dos Santos; Sebastian Harder; Rolf M Nüsing; Alexander Paulke; Holger Stark
Journal:  ACS Med Chem Lett       Date:  2012-08-08       Impact factor: 4.345

Review 4.  International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.

Authors:  Pertti Panula; Paul L Chazot; Marlon Cowart; Ralf Gutzmer; Rob Leurs; Wai L S Liu; Holger Stark; Robin L Thurmond; Helmut L Haas
Journal:  Pharmacol Rev       Date:  2015-07       Impact factor: 25.468

5.  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

6.  New Chemical Biology Tools for the Histamine Receptor Family.

Authors:  Yang Zheng; Gábor Wágner; Niels Hauwert; Xiaoyuan Ma; Henry F Vischer; Rob Leurs
Journal:  Curr Top Behav Neurosci       Date:  2022

7.  Novel chalcone-based fluorescent human histamine h(3) receptor ligands as pharmacological tools.

Authors:  Miriam Tomasch; J Stephan Schwed; Lilia Weizel; Holger Stark
Journal:  Front Syst Neurosci       Date:  2012-03-26
  7 in total

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