Update on the recent development of allosteric modulators for adenosine receptors and their therapeutic applications
S Pasquini, C Contri, M Cappello, PA Borea… - Frontiers in …, 2022 - frontiersin.org
Adenosine receptors (ARs) have been identified as promising therapeutic targets for
countless pathological conditions, spanning from inflammatory diseases to central nervous …
countless pathological conditions, spanning from inflammatory diseases to central nervous …
[HTML][HTML] Coffee effectively attenuates impaired attention in ADORA2A C/C-allele carriers during chronic sleep restriction
DM Baur, D Lange, EM Elmenhorst… - Progress in Neuro …, 2021 - Elsevier
Many people consume coffee to attenuate increased sleepiness and impaired vigilance and
attention due to insufficient sleep. We investigated in genetically caffeine sensitive men and …
attention due to insufficient sleep. We investigated in genetically caffeine sensitive men and …
[HTML][HTML] Anti-parkinsonian activity of the adenosine A2A receptor antagonist/inverse agonist KW-6356 as monotherapy in MPTP-treated common marmosets
Y Ohno, E Okita, M Kawai-Uchida, N Fukuda… - European Journal of …, 2023 - Elsevier
KW-6356 is a novel adenosine A 2A receptor antagonist/inverse agonist that not only blocks
binding of adenosine to adenosine A 2A receptor but also inhibits the constitutive activity of …
binding of adenosine to adenosine A 2A receptor but also inhibits the constitutive activity of …
Adenosine A2A Receptor Blockade Provides More Effective Benefits at the Onset Rather than after Overt Neurodegeneration in a Rat Model of Parkinson's Disease
ACL Nunes, M Carmo, A Behrenswerth… - International journal of …, 2024 - mdpi.com
Adenosine A2A receptor (A2AR) antagonists are the leading nondopaminergic therapy to
manage Parkinson's disease (PD) since they afford both motor benefits and neuroprotection …
manage Parkinson's disease (PD) since they afford both motor benefits and neuroprotection …
Unmasking allosteric-binding sites: novel targets for GPCR drug discovery
V Casadó-Anguera, V Casadó - Expert Opinion on Drug Discovery, 2022 - Taylor & Francis
Introduction Unexpected non-apparent and hidden allosteric-binding sites are non-classical
and non-apparent allosteric centers in 3-D X-ray protein structures until orthosteric or …
and non-apparent allosteric centers in 3-D X-ray protein structures until orthosteric or …
[HTML][HTML] The adenosine A2A receptor antagonist/inverse agonist, KW-6356 enhances the anti-parkinsonian activity of L-DOPA with a low risk of dyskinesia in MPTP …
Y Ohno, E Okita, M Kawai-Uchida, Y Shoukei… - Journal of …, 2023 - Elsevier
The adenosine A 2A receptor antagonist/inverse agonist, KW-6356 has been shown to be
effective in Parkinson's disease (PD) patients as monotherapy and as an adjunct therapy to …
effective in Parkinson's disease (PD) patients as monotherapy and as an adjunct therapy to …
“Dual Anta-Inhibitors” of the A2A Adenosine Receptor and Casein Kinase CK1delta: Synthesis, Biological Evaluation, and Molecular Modeling Studies
A Spinaci, M Buccioni, D Catarzi, C Cui, V Colotta… - Pharmaceuticals, 2023 - mdpi.com
Based on a screening of a chemical library of A2A adenosine receptor (AR) antagonists, a
series of di-and tri-substituted adenine derivatives were synthesized and tested for their …
series of di-and tri-substituted adenine derivatives were synthesized and tested for their …
The MPTP-lesioned marmoset model of Parkinson's disease: proposed efficacy thresholds that may potentially predict successful clinical trial results
F Beaudry, P Huot - Journal of Neural Transmission, 2020 - Springer
Abstract The 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP)-lesioned common
marmoset has been used extensively to model Parkinson's disease, l-3, 4 …
marmoset has been used extensively to model Parkinson's disease, l-3, 4 …
Role of adenosine A2A receptors in the loss of consciousness induced by propofol anesthesia
M Guo, J Wang, Y Yuan, L Chen, J He… - Journal of …, 2023 - Wiley Online Library
The mechanism of propofol‐anesthesia‐induced loss of consciousness (LOC) remains
largely unknown. We speculated that the adenosine A2A receptor serves as a vital …
largely unknown. We speculated that the adenosine A2A receptor serves as a vital …
Endoplasmic reticulum-based calcium dysfunctions in synucleinopathies
Neuronal calcium dyshomeostasis has been associated to Parkinson's disease (PD)
development based on epidemiological studies on users of calcium channel antagonists …
development based on epidemiological studies on users of calcium channel antagonists …