Adenosine receptors selective ligands

Rivkees SA, Lasbury ME, Barbahalya H. Identification of domains of the human Ai adenosine receptor that are important for binding receptor subtype selective ligands using chimeric Ai/A2 adenosine receptors. J Biol Chem 1995 270 20485-20490. 

Gao Z-G, Kim S-K, Biadatti T, Chen W, Lee K, Barak D, Kim S-G, Johnson CR, Jacobson KA (2002) Structural determinants of A3 adenosine receptor activation nucleoside ligands at the agonist/antagonist boundary. J Med Chem 445 4471-4484 Gao Z-G, Blaustein JB, Gross AS, Melman N, Jacobson KA (2003) M -Substituted adenosine derivatives selectivity, efficacy, and species differences at A3 adenosine receptors. Biochem Pharmacol 65 1675-1684... 

Jacobson KA, von Lubitz DKJE, Daly JW, Fredholm BB (1996) Adenosine receptor ligands differences with acute and chronic treatment. Trends Pharmacol Sci 17(3) 108-113 Jacobson KA, Ji X-D, Li AH, Melman N, Siddiqui MA, Shin KJ, Marquez VE, Ravi RG (2000) Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem 43(ll) 2196-2203... 

Okamura et al. (2002, 2004a) recently reported the study of a new series of l,2,4-triazolo[5,l-i]purines. This research group highlighted the structural similarity between the new class of compounds and the triazoloquinazoline derivatives and consequently evaluated the corresponding A3 adenosine receptor affinities. These investigations led to potent and selective hA3 ligands, the most potent of which are reported in Fig. 7.12 (19, 20), in particular 5-n-butyl-8-(4-n-propoxyphenyl)-3H- 1,2,4 triazolo 5,1 -ilpurinc 20 exhibited the best selectivity profile of this series... 

Lenzi O, Colotta V, Catarzi D, Varano F, Filacchioni G, Martini C, Trincavelli L, Ciampi O, Varani K, Marighetti F, Morizzo E, Moro S (2006) 4-Amido-2-aryl-l, 2, 4-triazolo[4, 3-a] quinoxalin-l-ones as new potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies. J Med Chem 49 3916-3925... 

Volpini R, Dal Ben D, Lambertucci C, Taffi S, Vittori S, Klotz KN, Cristalli G (2007) N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor. J Med Chem 50(6) 1222-1230... 

Subtype-selective agonists and antagonists of the adenosine receptors have been developed (Jacobson and Gao 2006). Table 13.1 shows the affinity at the human subtypes of selective ligand probes of the A, A2a, and A3 receptors used in skeletal muscle studies. Two agonists of the receptor are listed Cl-IBMECA is a 9-riboside... 

Table 13.1 Structures and addinities at four subtypes of adenosine receptors of selective ligands used in studying skeletal muscle protection. 

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