Literature DB >> 24900647

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

Miriam Tomasch1, J Stephan Schwed1, Alexander Paulke2, Holger Stark1.   

Abstract

A piperidine-based lead structure for the human histamine H3 receptor (hH3R) was coupled with the BODIPY fluorophore and resulted in a strong green fluorescent (quantum yield, 0.92) hH3R ligand with affinity in the nanomolar concentration range (K i hH3R = 6.51 ± 3.31 nM), named Bodilisant. Screening for affinities at histamine and dopamine receptor subtypes showed high hH3R preference. Bodilisant was used for visualization of hH3R in hH3R overexpressing HEK-293 cells with fluorescence confocal laser scanning microscopy. In addition, in native human brain tissues, Bodilisant showed clear and displaceable images of labeled hH3R.

Entities:  

Keywords:  BODIPY; GPCR; H3 receptor; HEK-293 cells; displacement; fluorescence confocal laser scanning microscopy; histamine; nonimidazole derivative; pharmacological tool; tissue labeling

Year:  2012        PMID： 24900647      PMCID： PMC4027500          DOI： 10.1021/ml300383n

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  34 in total

1.  Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.

Authors:  X Ligneau; S Morisset; J Tardivel-Lacombe; F Gbahou; C R Ganellin; H Stark; W Schunack; J C Schwartz; J M Arrang
Journal:  Br J Pharmacol       Date:  2000-12       Impact factor: 8.739

2.  GPCR targeted library design: novel dopamine D3 receptor ligands.

Authors:  A Böcker; B C Sasse; M Nietert; H Stark; G Schneider
Journal:  ChemMedChem       Date:  2007-07       Impact factor: 3.466

3.  Synthesis and pharmacological characterization of novel fluorescent histamine H2-receptor ligands derived from aminopotentidine.

Authors:  Sheng-Xue Xie; Georgiana Petrache; Erich Schneider; Qi-Zhuang Ye; Günther Bernhardt; Roland Seifert; Armin Buschauer
Journal:  Bioorg Med Chem Lett       Date:  2006-05-30       Impact factor: 2.823

4.  Histamine H1, H3 and H4 receptors are involved in pruritus.

Authors:  K Rossbach; C Nassenstein; M Gschwandtner; D Schnell; K Sander; R Seifert; H Stark; M Kietzmann; W Bäumer
Journal:  Neuroscience       Date:  2011-06-13       Impact factor: 3.590

Review 5.  Histamine H3 receptor antagonists go to clinics.

Authors:  Kerstin Sander; Tim Kottke; Holger Stark
Journal:  Biol Pharm Bull       Date:  2008-12       Impact factor: 2.233

6.  Pharmacology and direct visualisation of BODIPY-TMR-CGP: a long-acting fluorescent beta2-adrenoceptor agonist.

Authors:  Jillian G Baker; Ian P Hall; Stephen J Hill
Journal:  Br J Pharmacol       Date:  2003-05       Impact factor: 8.739

7.  Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.

Authors:  Y von Coburg; T Kottke; L Weizel; X Ligneau; H Stark
Journal:  Bioorg Med Chem Lett       Date:  2008-09-07       Impact factor: 2.823

8.  Highly potent fluorescence-tagged nonimidazole histamine H3 receptor ligands.

Authors:  Michael Amon; Xavier Ligneau; Jean-Claude Camelin; Isabelle Berrebi-Bertrand; Jean-Charles Schwartz; Holger Stark
Journal:  ChemMedChem       Date:  2007-05       Impact factor: 3.466

9.  Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.

Authors:  Chouaib Tahtaoui; Isabelle Parrot; Philippe Klotz; Fabrice Guillier; Jean-Luc Galzi; Marcel Hibert; Brigitte Ilien
Journal:  J Med Chem       Date:  2004-08-12       Impact factor: 7.446

Review 10.  Histamine receptor subtypes: a century of rational drug design.

Authors:  Miriam Walter; Holger Stark
Journal:  Front Biosci (Schol Ed)       Date:  2012-01-01
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  8 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

Review 2.  Pharmacological Characterization of Human Histamine Receptors and Histamine Receptor Mutants in the Sf9 Cell Expression System.

Authors:  Erich H Schneider; Roland Seifert
Journal:  Handb Exp Pharmacol       Date:  2017

3.  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

4.  Chemical Probes for Histamine Receptor Subtypes.

Authors:  Markus Falkenstein; Milica Elek; Holger Stark
Journal:  Curr Top Behav Neurosci       Date:  2022

5.  Drug-likeness approach of 2-aminopyrimidines as histamine H3 receptor ligands.

Authors:  Bassem Sadek; Annemarie Schreeb; Johannes Stephan Schwed; Lilia Weizel; Holger Stark
Journal:  Drug Des Devel Ther       Date:  2014-09-19       Impact factor: 4.162

6.  Non-imidazole-based histamine H3 receptor antagonists with anticonvulsant activity in different seizure models in male adult rats.

Authors:  Bassem Sadek; Ali Saad; Gniewomir Latacz; Kamil Kuder; Agnieszka Olejarz; Tadeusz Karcz; Holger Stark; Katarzyna Kieć-Kononowicz
Journal:  Drug Des Devel Ther       Date:  2016-11-25       Impact factor: 4.162

7.  The Histamine H3 Receptor Antagonist E159 Reverses Memory Deficits Induced by Dizocilpine in Passive Avoidance and Novel Object Recognition Paradigm in Rats.

Authors:  Alaa Alachkar; Dorota Łażewska; Katarzyna Kieć-Kononowicz; Bassem Sadek
Journal:  Front Pharmacol       Date:  2017-10-12       Impact factor: 5.810

Review 8.  Recent Progress of Fluorescence Sensors for Histamine in Foods.

Authors:  Gan Wu; Xilin Dou; Dapeng Li; Shihan Xu; Jicheng Zhang; Zhaoyang Ding; Jing Xie
Journal:  Biosensors (Basel)       Date:  2022-03-04
  8 in total

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