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New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
TLDR
Five non-adenosine agonists are presented, including 2-amino-4-(4-hydroxyphenyl)-6-(1H-imidazol-2-ylmethylsulfanyl)pyridine-3,5-dicarbonitrile, which is a high-efficacy partial agonist and lacking selectivity versus the A(1) and A(2A) subtypes.
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
TLDR
In general, distal modifications of the N5-substituent were highly modulatory to potency and selectivity at adenosine receptors, as determined in radioligand binding assays at rat brain A1 and A2A receptors and at recombinant human A3 receptors.
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
TLDR
It is concluded that the presence of at least one furan group rather than phenyl is beneficial for high affinity on the A 2A adenosine receptor.
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
TLDR
Two novel series of pyrimidines are synthesized, possessing good potency at the adenosine A1 receptor and desirable PSA values, and a restriction related to its polar surface area is proposed to achieve a compound that may act at the CNS.
N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors.
TLDR
The synthesis and biological evaluation of N6, C8-disubstituted derivatives ofAdenosine as potential partial agonists for adenosine receptors is described, with results that suggest lower intrinsic activities than the prototypic full agonist N6-cyclopentyladenosine on the decrease in heart rate in conscious, normotensive rats.
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
TLDR
A series of nonadenosine ligands selective for the adenosine A(1) receptor with an extraordinary pharmacological profile is presented, showing full agonistic behavior comparable with the reference compound CPA while also displaying comparable receptor binding affinity.
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.
TLDR
The most selective, high-affinity human adenosine A(1) receptor agonist was the disubstituted compound N(6)-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA).
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.
TLDR
New N,5'-di- and N,2,5-trisubstituted adenosine derivatives were synthesized in good overall yields and showed partial agonistic effects in both the cAMP and [35S]GTPgammaS assays, although more marked in the latter assay.
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