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A2A adenosine receptor agonists, antagonists, inverse agonists and partial agonists

2023
The Gs-coupled A2A adenosine receptor (A2AAR) has been explored extensively as a pharmaceutical target, which has led to numerous clinical trials. However, only one selective A2AAR agonist (regadenoson, Lexiscan) and one selective A2AAR antagonist (istradefylline, Nouriast) have been approved by the FDA, as a pharmacological agent for myocardial ...
Kenneth A, Jacobson   +2 more
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Calcium-Agonists

Journal of Molecular and Cellular Cardiology, 1986
In contrast to nifedipine-like calcium antagonists, calcium agonistic 1,4-dihydropyridines have vasoconstricting and positive inotropic properties. BAY K 8644 has become the prototype of this new class. Its enantiomers show opposite effects on the calcium channel: one acts as a calcium agonist with the pharmacological profile of the racemic compound ...
M, Bechem, M, Schramm
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In vitro characterization of agonist, antagonist, inverse agonist and agonist/antagonist benzodiazepines

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 1984
The efficacy of coupling between the benzodiazepine receptor and chloride channel as well as the coupling to the GABA receptor is differentially affected by different benzodiazepine ligands. In general, the order of efficacy with regard to allosteric effects of benzodiazepine ligands on the chloride channel ([35S]TBPS) and GABA receptor ([3H]muscimol),
P Loo   +3 more
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