History and perspectives of A2A adenosine receptor antagonists as potential therapeutic agents (Q38395423)

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scientific article published on 27 March 2015

Language	Label	Description	Also known as
English	History and perspectives of A2A adenosine receptor antagonists as potential therapeutic agents	scientific article published on 27 March 2015

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scholarly article

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Europe PubMed Central

PubMed publication ID

2 September 2017

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Europe PubMed Central

History and perspectives of A2A adenosine receptor antagonists as potential therapeutic agents (English)

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Europe PubMed Central

PubMed publication ID

2 September 2017

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Delia Preti

1

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author name string

Pier Giovanni Baraldi

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Europe PubMed Central

PubMed publication ID

2 September 2017

Allan R Moorman

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Europe PubMed Central

PubMed publication ID

2 September 2017

Pier Andrea Borea

4

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Europe PubMed Central

PubMed publication ID

2 September 2017

Katia Varani

5

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Europe PubMed Central

PubMed publication ID

2 September 2017

publication date

27 March 2015

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Europe PubMed Central

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2 September 2017

Medicinal Research Reviews

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Europe PubMed Central

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2 September 2017

35

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Europe PubMed Central

PubMed publication ID

2 September 2017

4

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Europe PubMed Central

PubMed publication ID

2 September 2017

790-848

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Europe PubMed Central

PubMed publication ID

2 September 2017

Adenosine receptors as drug targets

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

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A2A adenosine receptor overexpression and functionality, as well as TNF-alpha levels, correlate with motor symptoms in Parkinson's disease

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Aspects of the general biology of adenosine A2A signaling.

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GPCR 3D homology models for ligand screening: lessons learned from blind predictions of adenosine A2a receptor complex

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Structure of an agonist-bound human A2A adenosine receptor

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Adenosine A2A receptor signaling and golf assembly show a specific requirement for the gamma7 subtype in the striatum

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Signalling from adenosine receptors to mitogen-activated protein kinases

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Dimerization: an emerging concept for G protein-coupled receptor ontogeny and function

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Production of functional recombinant G-protein coupled receptors for heteromerization studies

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Homodimerization of adenosine A2A receptors: qualitative and quantitative assessment by fluorescence and bioluminescence energy transfer

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Useful pharmacological parameters for G-protein-coupled receptor homodimers obtained from competition experiments. Agonist-antagonist binding modulation.

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Regulation of immune cells by local-tissue oxygen tension: HIF1 alpha and adenosine receptors

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Neuroprotective potential of adenosine A2A and cannabinoid CB1 receptor antagonists in an animal model of Parkinson disease.

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Pre-synaptic adenosine A2A receptors control cannabinoid CB1 receptor-mediated inhibition of striatal glutamatergic neurotransmission.

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Inhibition of monoamine oxidase B by selective adenosine A2A receptor antagonists

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Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.

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2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization

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https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Discovery of nonxanthine adenosine A2A receptor antagonists for the treatment of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

7-Amino-2-phenylpyrazolo[4,3-d]pyrimidine derivatives: structural investigations at the 5-position to target human A₁ and A(2A) adenosine receptors. Molecular modeling and pharmacological studies

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

A novel conjugated agent between dopamine and an A2A adenosine receptor antagonist as a potential anti-Parkinson multitarget approach

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Adenosine A2A receptor-antagonist/dopamine D2 receptor-agonist bivalent ligands as pharmacological tools to detect A2A-D2 receptor heteromers

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Scaffold Decoration at Positions 5 and 8 of 1,2,4-Triazolo[1,5-c]Pyrimidines to Explore the Antagonist Profiling on Adenosine Receptors: A Preliminary Structure–Activity Relationship Study

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthetic studies on selective adenosine A2A receptor antagonists. Part II: synthesis and structure-activity relationships of novel benzofuran derivatives

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthesis of novel 7-imino-2-thioxo-3,7-dihydro-2H-thiazolo [4,5-d] pyrimidine derivatives as adenosine A2A receptor antagonists.

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Benzothiazinones: a novel class of adenosine receptor antagonists structurally unrelated to xanthine and adenine derivatives

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Identification of novel adenosine A(2A) receptor antagonists by virtual screening.

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Optimization of 6-heterocyclic-2-(1H-pyrazol-1-yl)-N-(pyridin-2-yl)pyrimidin-4-amine as potent adenosine A2A receptor antagonists for the treatment of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Discovery of 1,2,4-Triazine Derivatives as Adenosine A 2A Antagonists using Structure Based Drug Design

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinson's disease and cognition

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Brain adenosine A2A receptor occupancy by a novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: relationship to anticataleptic effect

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

A novel adenosine A(1) and A(2A) receptor antagonist ASP5854 ameliorates motor impairment in MPTP-treated marmosets: comparison with existing anti-Parkinson's disease drugs

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

The novel adenosine A2A antagonist Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Emerging therapies for Parkinson's disease: from bench to bedside.

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Epidemiology of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Novel pharmacological targets for the treatment of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Levodopa in the treatment of Parkinson's disease: current controversies

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Istradefylline: first global approval

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Adenosine A(2A) receptor antagonist treatment of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Adenosine A2A receptor antagonist istradefylline (KW-6002) reduces "off" time in Parkinson's disease: a double-blind, randomized, multicenter clinical trial (6002-US-005).

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Clinical efficacy of istradefylline (KW-6002) in Parkinson's disease: a randomized, controlled study

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Adenosine A2A receptor antagonist istradefylline reduces daily OFF time in Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Levodopa-carbidopa intestinal gel in advanced Parkinson's disease open-label study: interim results

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

A long-term study of istradefylline in subjects with fluctuating Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in rats

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

ST 1535: a preferential A2A adenosine receptor antagonist

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Future treatments for Parkinson's disease: surfing the PD pipeline

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Quantification of indirect pathway inhibition by the adenosine A2a antagonist SYN115 in Parkinson disease.

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

An open-label, positron emission tomography study to assess adenosine A2A brain receptor occupancy of vipadenant (BIIB014) at steady-state levels in healthy male volunteers

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Safety, tolerability and pharmacokinetics after single and multiple doses of preladenant (SCH420814) administered in healthy subjects

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Preladenant, a selective adenosine A₂A receptor antagonist, is not associated with QT/QTc prolongation

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Long-term safety and efficacy of preladenant in subjects with fluctuating Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Adenosine A(2A) receptor antagonists as Positron Emission Tomography (PET) tracers

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Adenosine 2A receptor occupancy by tozadenant and preladenant in rhesus monkeys

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Pyrazolo[4,3-e][1,2,4]Triazolo[1,5-c]Pyrimidine Template: Organic and Medicinal Chemistry Approach

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FMED.21344

21 January 2018

Identifiers

10.1002/MED.21344

1 reference

Europe PubMed Central

PubMed publication ID

2 September 2017

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

2 September 2017

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