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

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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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.

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Titolo:	Novel N-6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A(3) adenosine receptors
Autori:	BARALDI, Pier Giovanni CACCIARI, Barbara SPALLUTO G JI XD OLAH ME STILES G DIONISOTTI S ZOCCHI C ONGINI E JACOBSON KA mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	1996
Rivista:	JOURNAL OF MEDICINAL CHEMISTRY
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.
Handle:	http://hdl.handle.net/11392/516801
Appare nelle tipologie:	03.1 Articolo su rivista

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