Title compds. I (R = Et, R1 = H, CF3, MeO, F, Cl, I, 4-​Me, 3-​Br; R = Me, R1 = 4-​MeO, 3-​Cl) were synthesized and tested for their affinity at A1 and A2A adenosine receptors in rat brain membranes and at cloned rat A3 receptors from stably transfected CHO cells. N6-​[(2-​chlorophenyl)​carbamoyl]​-​, N6-​[(3-​chlorophenyl)​carbamoyl]​-​, and N6-​[(4-​methoxyphenyl)​carbamoyl]​adenosine-​5'-​ethyluronamide (II) had affinity at A3 receptors in the low nanomolar range (Ki values <10 nM)​. In CHO cells stably transfected with the rat A3 receptor, II was a full agonist in inhibiting adenylate cyclase activity. The present study represents the first example of N6-​acyl-​substituted adenosine analogs having high affinity at adenosine receptors and, in particular, at the A3 receptor subtype.

Novel N-6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A(3) adenosine receptors

BARALDI, Pier Giovanni;CACCIARI, Barbara;
1996

Abstract

Title compds. I (R = Et, R1 = H, CF3, MeO, F, Cl, I, 4-​Me, 3-​Br; R = Me, R1 = 4-​MeO, 3-​Cl) were synthesized and tested for their affinity at A1 and A2A adenosine receptors in rat brain membranes and at cloned rat A3 receptors from stably transfected CHO cells. N6-​[(2-​chlorophenyl)​carbamoyl]​-​, N6-​[(3-​chlorophenyl)​carbamoyl]​-​, and N6-​[(4-​methoxyphenyl)​carbamoyl]​adenosine-​5'-​ethyluronamide (II) had affinity at A3 receptors in the low nanomolar range (Ki values <10 nM)​. In CHO cells stably transfected with the rat A3 receptor, II was a full agonist in inhibiting adenylate cyclase activity. The present study represents the first example of N6-​acyl-​substituted adenosine analogs having high affinity at adenosine receptors and, in particular, at the A3 receptor subtype.
Baraldi, Pier Giovanni; Cacciari, Barbara; Spalluto, G; Ji, Xd; Olah, Me; Stiles, G; Dionisotti, S; Zocchi, C; Ongini, E; Jacobson, Ka
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11392/516801
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