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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.
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.
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
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.
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
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.
Non‐Xanthine Antagonists for the Adenosine A1 Receptor
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
8-cyclopentyl-2,6-diphenylpurine (31, LUF 5962) has been shown to be very promising with an affinity of 0.29 nM at the human adenosine A(1) receptor.
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
A refined pharmacophore model for antagonists of the human adenosine A1 receptor is developed, based on features of known pyrimidine and purine derivatives, which assisted in synthesizing a series of 1-deazapurines with consistently high affinity as inverse agonists for the adenosines A1 receptors.
Novel ligands for the human adenosine A1 receptor
This research describes the quest to create 'super-caffeines', substances that only produce the desired effects of caffeine, and unlike caffeine, substances that should only have to be taken in