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The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist.
TLDR
Data show that SCH 58261 is a potent and selective non-xanthine A2a adenosine antagonist which has competitive properties in biological responses mediated by this receptor subtype.
Cardioprotective effects of adenosine A1 and A2A receptor agonists in the isolated rat heart.
TLDR
Findings indicate that both A1 and A2A adenosine receptors are involved in protecting the myocardium against ischemia and reperfusion in isolated rat heart, even if through different mechanisms.
Prolonged exposure to 5'-N-ethylcarboxamidoadenosine (NECA) does not affect the adenosine A2A-mediated vasodilation in porcine coronary arteries.
TLDR
Results indicate that prolonged stimulation of A2A receptors does not lead to loss of functional response, suggesting that this receptor subtype does not desensitize after prolonged stimulation by agonists.
2-Alkynyl derivatives of adenosine-5'-N-ethyluronamide: selective A2 adenosine receptor agonists with potent inhibitory activity on platelet aggregation.
TLDR
Introduction of an a-hydroxyl group in the alkynyl side chain caused a greater increase in antiaggregatory activity than either NECA or HE-NECA, resulting in the most potent inhibitors of platelet aggregation so far known in the nucleoside series.
2-Aralkynyl and 2-heteroalkynyl derivatives of adenosine-5'-N-ethyluronamide as selective A2a adenosine receptor agonists.
TLDR
The structure-activity relationships derived for the 2-alkynyl-substituted ribose uronamides would indicate that potentiation of A2a receptor affinity could be obtained by aromatic rings not conjugated with the triple bond or by heteroaromatic groups.
Pharmacology of the new selective A2a adenosine receptor agonist 2-hexynyl-5'-N-ethylcarboxamidoadenosine.
TLDR
The pharmacological profile of 2-hexynyl-5'-N-ethylcarboxamidoadenosine (2HE-NECA, CAS 141018-30-6), a new selective A2a adenosine receptor agonist, was characterized and showed a good A 2a vs A1 receptor selectivity in brain tissues of both animal species.
2-Alkynyl derivatives of adenosine-5'-N-ethyluronamide: selective A2 adenosine receptor agonists with potent inhibitory activity on platelet aggregation.
TLDR
Introduction of an alpha-hydroxyl group in the alkynyl side chain caused a greater increase in antiaggregatory activity than either NECA or HE-NECA, resulting in the most potent inhibitors of platelet aggregation so far known in the nucleoside series.
Effects of the new A2 adenosine receptor antagonist 8FB‐PTP, an 8 substituted pyrazolo‐triazolo‐pyrimidine, on in vitro functional models
TLDR
The in vitro pharmacological profile of putative A2 adenosine antagonists provided a basis to reduce, by further chemical modifications, the affinity at A1 receptor and therefore enhance A2 receptor selectivity.
Effects of selective A1 and A2 adenosine receptor agonists on cardiovascular tissues
TLDR
Positive chronotropic and vasodilating properties of new selective A1 and A2 adenosine agonists such as CCPA and 2-hexynyl-5′-N-ethyl-carboxamidoadenosine as compared with referenceAdenosine analogues support that A1 receptors are involved in depressing cardiac activity and A 2 receptors in inducing vasorelaxation.
Pharmacology of the highly selective A1 adenosine receptor agonist 2-chloro-N6-cyclopentyladenosine.
The pharmacological profile of 2-chloro-N6-cyclopentyladenosine (CCPA, CAS 37739-05-2), a highly selective A1 adenosine receptor agonist, was characterized. Its effects were compared with those of
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