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 …

T Mihara, K Mihara, J Yarimizu, Y Mitani… - … of Pharmacology and …, 2007 - ASPET
Central adenosine A2A receptor is a promising target for drugs to treat Parkinson's disease
(PD), and the central blockade of adenosine A1 receptor improves cognitive function. In the …

JNJ-40255293, a Novel Adenosine A2A/A1 Antagonist with Efficacy in Preclinical Models of Parkinson's Disease

JR Atack, BC Shook, S Rassnick… - ACS Chemical …, 2014 - ACS Publications
Adenosine A2A antagonists are believed to have therapeutic potential in the treatment of
Parkinson's disease (PD). We have characterized the dual adenosine A2A/A1 receptor …

In Vivo Characterization of a Dual Adenosine A2A/A1 Receptor Antagonist in Animal Models of Parkinson's Disease

BC Shook, S Rassnick, MC Osborne… - Journal of medicinal …, 2010 - ACS Publications
The in vivo characterization of a dual adenosine A2A/A1 receptor antagonist in several
animal models of Parkinson's disease is described. Discovery and scale-up syntheses of …

A new ethyladenine antagonist of adenosine A2A receptors: Behavioral and biochemical characterization as an antiparkinsonian drug

A Pinna, E Tronci, N Schintu, N Simola, R Volpini… - …, 2010 - Elsevier
Adenosine A2A receptor antagonists have emerged as an attractive non-dopaminergic
target in clinical trials aimed at evaluating improvement in motor deficits in Parkinson's …

Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's …

X Zhang, JE Tellew, Z Luo, M Moorjani… - Journal of medicinal …, 2008 - ACS Publications
4-Acetylamino-2-(3, 5-dimethylpyrazol-1-yl)-pyrimidines bearing substituted pyridyl groups
as C-6 substituents were prepared as selective adenosine hA2A receptor antagonists for the …

Distribution of adenosine A2A receptor antagonist KW-6002 and its effect on gene expression in the rat brain

S Aoyama, K Koga, A Mori, H Miyaji, S Sekine, H Kase… - Brain research, 2002 - Elsevier
A novel adenosine A2A receptor selective antagonist, KW-6002 [(E)-1, 3-diethyl-8-(3, 4-
dimethoxystyryl)-7-methyl-3, 7-dihydro-1H-purine-2, 6-dione], possesses antiparkinsonian …

Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP

S Shiozaki, S Ichikawa, J Nakamura, S Kitamura… - …, 1999 - Springer
Abstract Rationale: Current treatment of Parkinson's disease (PD) is based on dopamine
replacement therapy, but this leads to long term complications, including dyskinesia …

A novel adenosine A1 and A2A receptor antagonist ASP5854 ameliorates motor impairment in MPTP-treated marmosets: Comparison with existing anti-Parkinson's …

T Mihara, A Iwashita, N Matsuoka - Behavioural brain research, 2008 - Elsevier
Recent evidence indicates that adenosine A2A receptor antagonists hold therapeutic
potential for the treatment of Parkinson's disease (PD). A study on the novel adenosine A1 …

Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors

T Maemoto, M Tada, T Mihara, N Ueyama… - Journal of …, 2004 - jstage.jst.go.jp
Adenosine A1 receptors in the brain are believed to play an important role in brain
functioning. We have discovered a novel adenosine A1 receptor antagonist, FR194921 (2-(1 …

Design and Characterization of Optimized Adenosine A2A/A1 Receptor Antagonists for the Treatment of Parkinson's Disease

BC Shook, S Rassnick, N Wallace… - Journal of medicinal …, 2012 - ACS Publications
The design and characterization of two, dual adenosine A2A/A1 receptor antagonists in
several animal models of Parkinson's disease is described. Compound 1 was previously …