Literature DB >> 19362836

Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.

Roger J Gillespie1, Samantha J Bamford, Suneel Gaur, Allan M Jordan, Joanne Lerpiniere, Howard L Mansell, Gemma C Stratton.   

Abstract

A novel series of antagonists of the human A(2A) receptor have been identified and have been shown to display good potency and high degrees of selectivity over other receptor sub-types. Displaying in vivo potency in commonly used disease models and high oral bio-availability, this class of compounds may serve as clinically useful treatments for the relief of the symptoms associated with Parkinson's disease.

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Year:  2009        PMID: 19362836     DOI: 10.1016/j.bmcl.2009.03.142

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


  4 in total

Review 1.  Adenosine A(2A) Receptor Antagonists and Parkinson's Disease.

Authors:  Brian C Shook; Paul F Jackson
Journal:  ACS Chem Neurosci       Date:  2011-06-21       Impact factor: 4.418

2.  Inhibitors of membranous adenylyl cyclases with affinity for adenosine receptors.

Authors:  Karl-Norbert Klotz; Sonja Kachler
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2015-12-14       Impact factor: 3.000

3.  Pharmacological and physiological characterization of the tremulous jaw movement model of parkinsonian tremor: potential insights into the pathophysiology of tremor.

Authors:  Lyndsey E Collins-Praino; Nicholas E Paul; Kristen L Rychalsky; James R Hinman; James J Chrobak; Patrick B Senatus; John D Salamone
Journal:  Front Syst Neurosci       Date:  2011-07-04

4.  Discovery of indolylpiperazinylpyrimidines with dual-target profiles at adenosine A2A and dopamine D2 receptors for Parkinson's disease treatment.

Authors:  Yi-Ming Shao; Xiaohua Ma; Priyankar Paira; Aaron Tan; Deron Raymond Herr; Kah Leong Lim; Chee Hoe Ng; Gopalakrishnan Venkatesan; Karl-Norbert Klotz; Stephanie Federico; Giampiero Spalluto; Siew Lee Cheong; Yu Zong Chen; Giorgia Pastorin
Journal:  PLoS One       Date:  2018-01-05       Impact factor: 3.240

  4 in total

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