Literature DB >> 20561786

Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.

Michael A Letavic1, Leah Aluisio, John R Atack, Pascal Bonaventure, Nicholas I Carruthers, Christine Dugovic, Anita Everson, Mark A Feinstein, Ian C Fraser, Kenway Hoey, Xiaohui Jiang, John M Keith, Tatiana Koudriakova, Perry Leung, Brian Lord, Timothy W Lovenberg, Kiev S Ly, Kirsten L Morton, S Timothy Motley, Diane Nepomuceno, Michele Rizzolio, Raymond Rynberg, Kia Sepassi, Jonathan Shelton.   

Abstract

The pre-clinical characterization of novel aryloxypyridine amides that are histamine H(3) receptor antagonists is described. These compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat brain. Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20561786     DOI： 10.1016/j.bmcl.2010.05.041

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


  6 in total

1.  Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.

Authors:  Michael A Letavic; Leah Aluisio; Richard Apodaca; Manoj Bajpai; Ann J Barbier; Anne Bonneville; Pascal Bonaventure; Nicholas I Carruthers; Christine Dugovic; Ian C Fraser; Michelle L Kramer; Brian Lord; Timothy W Lovenberg; Lilian Y Li; Kiev S Ly; Heather Mcallister; Neelakandha S Mani; Kirsten L Morton; Anthony Ndifor; S Diane Nepomuceno; Chennagiri R Pandit; Steven B Sands; Chandra R Shah; Jonathan E Shelton; Sandra S Snook; Devin M Swanson; Wei Xiao
Journal:  ACS Med Chem Lett       Date:  2015-03-13       Impact factor: 4.345

2.  Blockade of the brain histamine H3 receptor by JNJ-39220675: preclinical PET studies with [¹¹C]GSK189254 in anesthetized baboon.

Authors:  Jean Logan; Nicholas I Carruthers; Michael A Letavic; Steven Sands; Xiaohui Jiang; Colleen Shea; Lisa Muench; Youwen Xu; Pauline Carter; Payton King; Joanna S Fowler
Journal:  Psychopharmacology (Berl)       Date:  2012-05-22       Impact factor: 4.530

3.  JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats.

Authors:  Ruggero Galici; Amir H Rezvani; Leah Aluisio; Brian Lord; Edward D Levin; Ian Fraser; Jamin Boggs; Natalie Welty; James R Shoblock; S Timothy Motley; Michael A Letavic; Nicholas I Carruthers; Christine Dugovic; Timothy W Lovenberg; Pascal Bonaventure
Journal:  Psychopharmacology (Berl)       Date:  2010-11-18       Impact factor: 4.530

Review 4.  Therapeutic Potential of Histamine H3 Receptors in Substance Use Disorders.

Authors:  Patricia Di Ciano; Christian S Hendershot; Bernard Le Foll
Journal:  Curr Top Behav Neurosci       Date:  2022

5.  Histamine is required for H₃ receptor-mediated alcohol reward inhibition, but not for alcohol consumption or stimulation.

Authors:  J Vanhanen; S Nuutinen; M Lintunen; T Mäki; J Rämö; K Karlstedt; P Panula
Journal:  Br J Pharmacol       Date:  2013-09       Impact factor: 8.739

Review 6.  Cyclobutanes in Small-Molecule Drug Candidates.

Authors:  Marnix R van der Kolk; Mathilde A C H Janssen; Floris P J T Rutjes; Daniel Blanco-Ania
Journal:  ChemMedChem       Date:  2022-03-29       Impact factor: 3.540
  6 in total

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