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EnglishTitle 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: | |
| Data di pubblicazione: | 1996 |
| Rivista: | |
| 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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