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open access: yesJAMA Pediatr
europepmc   +1 more source
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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
openaire   +2 more sources

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
openaire   +2 more sources

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 L, Wood   +3 more
openaire   +2 more sources

Agonists, partial agonists, antagonists, inverse agonists and agonist/antagonists?

Trends in Pharmacological Sciences, 1987
The label placed on a drug influences its ultimate use. But interpretation ofin-vivo data has complicated the simple receptor theory of agonists and antagonists for certain classes of drugs.Terry Kenakin argues that clarification of such data — described in an extremely complex system — at a molecular level, will either obviate the need for terms such ...
openaire   +1 more source

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