Literature DB >> 19888872

Novel investigational adenosine A2A receptor antagonists for Parkinson's disease.

Annalisa Pinna1.   

Abstract

The development of non-dopaminergic therapies for Parkinson's disease (PD) has attracted much interest in recent years. Among new classes of drugs, adenosine A(2A) antagonists have emerged as the best candidates. BIIB014, preladenant and ST-1535 are new adenosine A(2A) antagonists currently in Phase I and II clinical trials for evaluation of their efficacy in patients with PD. All these compounds have been proven safe and well tolerated. Moreover, results from Phase II trials also demonstrate that BIIB014 and preladenant are effective in reducing the waking time spent in OFF state in patients at the late stage of PD treated with L-DOPA. BIIB014 is also efficacious as monotherapy in patients at the early stage of PD. Finally, ST-1535, at this time, displays a very promising potential in experimental models of PD and a safe profile in clinical studies. This review summarizes pharmacological data available on these three A(2A) antagonists, their effects in animal models of PD and their profiles in clinical trials.

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Year:  2009        PMID: 19888872     DOI: 10.1517/13543780903241615

Source DB:  PubMed          Journal:  Expert Opin Investig Drugs        ISSN: 1354-3784            Impact factor:   6.206


  28 in total

1.  Novel Alexa Fluor-488 labeled antagonist of the A(2A) adenosine receptor: Application to a fluorescence polarization-based receptor binding assay.

Authors:  Miklós Kecskés; T Santhosh Kumar; Lena Yoo; Zhan-Guo Gao; Kenneth A Jacobson
Journal:  Biochem Pharmacol       Date:  2010-05-11       Impact factor: 5.858

Review 2.  Adenosine A2A receptor antagonists in Parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued.

Authors:  Annalisa Pinna
Journal:  CNS Drugs       Date:  2014-05       Impact factor: 5.749

3.  Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold.

Authors:  T Santhosh Kumar; Shilpi Mishra; Francesca Deflorian; Lena S Yoo; Khai Phan; Miklos Kecskés; Angela Szabo; Bidhan Shinkre; Zhan-Guo Gao; William Trenkle; Kenneth A Jacobson
Journal:  Bioorg Med Chem Lett       Date:  2010-11-21       Impact factor: 2.823

Review 4.  Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.

Authors:  Marie Therese Armentero; Annalisa Pinna; Sergi Ferré; José Luis Lanciego; Christa E Müller; Rafael Franco
Journal:  Pharmacol Ther       Date:  2011-07-23       Impact factor: 12.310

Review 5.  International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.

Authors:  Bertil B Fredholm; Adriaan P IJzerman; Kenneth A Jacobson; Joel Linden; Christa E Müller
Journal:  Pharmacol Rev       Date:  2011-02-08       Impact factor: 25.468

Review 6.  Mechanisms underlying the onset and expression of levodopa-induced dyskinesia and their pharmacological manipulation.

Authors:  Mahmoud M Iravani; Peter Jenner
Journal:  J Neural Transm (Vienna)       Date:  2011-09-01       Impact factor: 3.575

7.  Immune Alterations in CD8+ T Cells Are Associated with Neuronal C-C and C-X-C Chemokine Receptor Regulation Through Adenosine A2A Receptor Signaling in a BTBR T+ Itpr3tf/J Autistic Mouse Model.

Authors:  Sheikh F Ahmad; Mushtaq A Ansari; Ahmed Nadeem; Saleh A Bakheet; Raish Mohammad; Sabry M Attia
Journal:  Mol Neurobiol       Date:  2017-04-18       Impact factor: 5.590

Review 8.  Hostile, hypoxia-A2-adenosinergic tumor biology as the next barrier to overcome for tumor immunologists.

Authors:  Michail V Sitkovsky; Stephen Hatfield; Robert Abbott; Bryan Belikoff; Dmitriy Lukashev; Akio Ohta
Journal:  Cancer Immunol Res       Date:  2014-07       Impact factor: 11.151

Review 9.  Adenosine receptors as drug targets--what are the challenges?

Authors:  Jiang-Fan Chen; Holger K Eltzschig; Bertil B Fredholm
Journal:  Nat Rev Drug Discov       Date:  2013-04       Impact factor: 84.694

10.  Rescuing the Corticostriatal Synaptic Disconnection in the R6/2 Mouse Model of Huntington's Disease: Exercise, Adenosine Receptors and Ampakines.

Authors:  Carlos Cepeda; Damian M Cummings; Miriam A Hickey; Max Kleiman-Weiner; Jane Y Chen; Joseph B Watson; Michael S Levine
Journal:  PLoS Curr       Date:  2010-09-20
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