Literature DB >> 12930154

A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.

Richard Apodaca1, Curt A Dvorak, Wei Xiao, Ann J Barbier, Jamin D Boggs, Sandy J Wilson, Timothy W Lovenberg, Nicholas I Carruthers.   

Abstract

4-(Aminoalkoxy)benzylamines were prepared and screened for in vitro activity at the human histamine H(3) receptor. Some members of this series exhibited subnanomolar binding affinities. Analogues in which one nitrogen atom was replaced with a methine group showed greatly reduced binding affinities. Six members of this series were found to be antagonists in a cell-based model of human histamine H(3) receptor activation. One member of this series, 1-[4-(3-piperidin-1-ylpropoxy)benzyl]piperidine (7b), was found to be a selective and potent human H(3) receptor antagonist.

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Year:  2003        PMID： 12930154     DOI： 10.1021/jm030185v

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  7 in total

Review 1.  Roles of histamine and its receptors in allergic and inflammatory bowel diseases.

Authors:  Hua Xie; Shao-Heng He
Journal:  World J Gastroenterol       Date:  2005-05-21       Impact factor: 5.742

2.  Histamine H3-receptor agonists and imidazole-based H3-receptor antagonists can be thermodynamically discriminated.

Authors:  E A Harper; J W Black
Journal:  Br J Pharmacol       Date:  2007-04-02       Impact factor: 8.739

3.  Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist.

Authors:  A J Barbier; C Berridge; C Dugovic; A D Laposky; S J Wilson; J Boggs; L Aluisio; B Lord; C Mazur; C M Pudiak; X Langlois; W Xiao; R Apodaca; N I Carruthers; T W Lovenberg
Journal:  Br J Pharmacol       Date:  2004-10-04       Impact factor: 8.739

4.  In vitro and in vivo pharmacological analysis of imidazole-free histamine H3 receptor antagonists: promising results for a brain-penetrating H3 blocker with weak anticholinesterase activity.

Authors:  Simona Bertoni; Vigilio Ballabeni; Lisa Flammini; Francesca Saccani; Giuseppe Domenichini; Giovanni Morini; Mara Comini; Mirko Rivara; Elisabetta Barocelli
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2008-05-22       Impact factor: 3.000

5.  Non-imidazole histamine H3 ligands: part V. synthesis and preliminary pharmacological investigation of 1-[2-thiazol-4-yl- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives.

Authors:  Roman Guryn; Marek Staszewski; Krzysztof Walczyński
Journal:  Med Chem Res       Date:  2012-11-29       Impact factor: 1.965

6.  4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H₃ Receptor Antagonist: Further Structure⁻Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation.

Authors:  Beata Olszewska; Anna Stasiak; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Rob Leurs; Krzysztof Walczyński
Journal:  Int J Mol Sci       Date:  2018-04-19       Impact factor: 5.923

7.  Improvement of the Prediction Power of the CoMFA and CoMSIA Models on Histamine H3 Antagonists by Different Variable Selection Methods.

Authors:  Jahan B Ghasemi; Hossein Tavakoli
Journal:  Sci Pharm       Date:  2012-05-24
  7 in total

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