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The adenosine receptor affinities and monoamine oxidase B inhibitory properties of sulfanylphthalimide analogues
(Elsevier, 2015)
Based on a report that sulfanylphthalimides are highly potent monoamine oxidase (MAO) B selective inhibitors, the present study examines the adenosine receptor affinities and MAO-B inhibitory properties of a series of 4- ...
1,3,7-Triethyl-substituted xanthines-possess nanomolar affinity for the adenosine A1 receptor
(Elsevier, 2015)
Adenosine A1 receptors are attracting great interest as drug targets for their role in cognitive deficits. Antagonism of the adenosine A1 receptor may offer therapeutic benefits in complex neurological diseases, such as ...
2-Aminopyrimidines as dual adenosine A1/A2A antagonists
(Elsevier, 2015)
In this study thirteen 2-aminopyrimidine derivatives were synthesised and screened as potential antagonists of adenosine A1 and A2A receptors in order to further investigate the structure activity relationships of this ...
C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range
(Springer, 2020)
To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones (15–36 and 37–41) and structurally related ...
Discovery of 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine derivatives as novel adenosine A1 and A2A receptor antagonists
(Elsevier, 2016)
Based on a previous report that a series of 8-(phenoxymethyl)-xanthines may be promising leads for the design of A1 adenosine receptor antagonists, selected novel and known 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine ...
Synthesis and evaluation of methoxy substituted 2-benzoyl-1-benzofuran derivatives as lead compounds for the development adenosine A1 and/or A2A receptor antagonists
(Elsevier, 2020)
A series of fourteen methoxy substituted 2-benzoyl-1-benzofuran derivatives were synthesised and their affinities determined for adenosine A1 and A2A receptors via radioligand binding assays to establish the structure ...
Methoxy substituted 2-benzylidene-1-indanone derivatives as A1 and/or A2A AR antagonists for the potential treatment of neurological conditions
(RSC, 2019)
A prior study reported on hydroxy substituted 2-benzylidene-1-indanone derivatives as A1 and/or A2A antagonists for the potential treatment of neurological conditions. A lead compound (1a) was identified with both A1 and ...
2-Benzylidene-1-indanone analogues as dual adenosine A1/A2a receptor antagonists for the potential treatment of neurological conditions
(Thieme, 2019)
Previous studies explored 2-benzylidine-1-tetralone derivatives as innovative adenosine A1 and A2A receptor antagonists for alternative non-dopaminergic treatment of Parkinson’s disease. This study’s aim is to investigate ...
The styrene metabolite, phenylglyoxylic acid, induces striatal-motor toxicity in the rat: influence of dose escalation/reduction over time
(Springer, 2011)
Exposure to the industrial solvent, styrene, induces locomotor and cognitive dysfunction in rats, and parkinsonian-like manifestations in man. The antipsychotic, haloperidol (HP), well known to induce striatal toxicity in ...
Deuterium isotope effects for the oxidation of 1-methyl-3phenyl-3pyrrolinyl analogues by monoamine oxidase B
(Elsevier, 2008)
The parkinsonian inducing agent, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), is a cyclic tertiary allylamine exhibiting good monoamine oxidase B (MAO-B) substrate properties. MAO-B catalyzes the ring α-carbon ...