Adenosine receptors and their ligands

KN Klotz - Naunyn-Schmiedeberg's archives of pharmacology, 2000 - Springer
The regulatory actions of adenosine are mediated via four subtypes of G protein-coupled
receptors distinguished as A 1, A 2A, A 2B and A 3 receptors. Their presence on basically …

Xanthines as adenosine receptor antagonists

BB Fredholm, CE Müller, KA Jacobson - Methylxanthines, 2011 - Springer
The natural plant alkaloids caffeine and theophylline were the first adenosine receptor (AR)
antagonists described in the literature. They exhibit micromolar affinities and are non …

Water-Soluble Phosphate Prodrugs of 1-Propargyl-8-styrylxanthine Derivatives, A2A-Selective Adenosine Receptor Antagonists

R Sauer, J Maurinsh, U Reith, F Fülle… - Journal of medicinal …, 2000 - ACS Publications
Water-soluble prodrugs of potent, A2A-selective adenosine receptor (AR) antagonists were
prepared. 8-(m-Bromostyryl)-3, 7-dimethyl-1-propargylxanthine (BS-DMPX, 11) and the …

Progress in the pursuit of therapeutic adenosine receptor antagonists

S Moro, ZG Gao, KA Jacobson… - Medicinal research …, 2006 - Wiley Online Library
Ever since the discovery of the hypotensive and bradycardiac effects of adenosine,
adenosine receptors continue to represent promising drug targets. First, this is due to the fact …

1,8-Disubstituted Xanthine Derivatives:  Synthesis of Potent A2B-Selective Adenosine Receptor Antagonists

AM Hayallah, J Sandoval-Ramírez… - Journal of medicinal …, 2002 - ACS Publications
3-Unsubstituted xanthine derivatives bearing a cyclopentyl or a phenyl residue in the 8-
position were synthesized and developed as A2B adenosine receptor antagonists …

Nucleoside transporters and immunosuppressive adenosine signaling in the tumor microenvironment: Potential therapeutic opportunities

T Kaur, B Weadick, TA Mace, K Desai, H Odom… - Pharmacology & …, 2022 - Elsevier
Adenosine compartmentalization has a profound impact on immune cell function by
regulating adenosine localization and, therefore, extracellular signaling capabilities, which …

A1 Adenosine Receptor Antagonists, Agonists, and Allosteric Enhancers

WF Kiesman, E Elzein, J Zablocki - Adenosine receptors in health and …, 2009 - Springer
Intense efforts of many pharmaceutical companies and academicians in the A 1 adenosine
receptor (AR) field have led to the discovery of clinical candidates that are antagonists …

The importance of the adenosine A2A receptor-dopamine D2 receptor interaction in drug addiction

M Filip, M Zaniewska, M Frankowska… - Current medicinal …, 2012 - ingentaconnect.com
Drug addiction is a serious brain disorder with somatic, psychological, psychiatric, socio-
economic and legal implications in the developed world. Illegal (eg, psychostimulants …

Binding of [3H] MSX-2 (3-(3-hydroxypropyl)-7-methyl-8-(m-methoxystyryl)-1-propargylxanthine) to rat striatal membranes—a new, selective antagonist radioligand for …

CE Müller, J Maurinsh, R Sauer - European journal of pharmaceutical …, 2000 - Elsevier
The present study describes the preparation and binding properties of a new, potent, and
selective A2A adenosine receptor (AR) antagonist radioligand,[3H] 3-(3-hydroxypropyl)-7 …

Inhibition of monoamine oxidase by indole and benzofuran derivatives

LHA Prins, JP Petzer, SF Malan - European Journal of Medicinal Chemistry, 2010 - Elsevier
Monoamine oxidase (MAO) is an important drug target for the treatment of neurological
disorders. A series of indole and benzofuran derivatives were synthesised and evaluated as …