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Table 2 Functional EC50 values for nucleoside monomers and dendrimer conjugates to activate the A1 AR ([35S]GTPγS binding and cAMP inhibition) and A3 AR (cAMP inhibition).a

From: Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates

Compound A1
([35S]GTPγS binding), EC50 (nM)
A1
(adenylyl cyclase), EC50 (nM)
A3
(adenylyl cyclase), EC50 (nM)
Nucleoside Monomers
1 94 ± 26 400 ± 80 100 ± 50
4 1300 ± 400 350 ± 20 140 ± 70
7 63 ± 14 89 ± 17 36 ± 13
Dendrimer Derivatives
11 50%b inactivec inactivec
12 190 ± 70 23 ± 10 25 ± 10
13 940 ± 70 54 ± 20 17 ± 2
15 < 10%b inactivec inactivec
16 2400 ± 1300 120 ± 1 14 ± 5
17 370 ± 190 260 ± 90 1.6 ± 0.4
  1. a. All experiments were performed using adherent CHO cells stably expressing the A1 or A3 AR. Binding of [35S]GTPγS and assays using a cAMP kit were carried out as described in methods. Values are expressed as EC50 values (mean ± SEM, n = 3) or as displacement of the radioligand at 10 μM. b. Percent of [35S]GTPγS binding at 10 μM compared to full agonist. c. Compound produced less than 20% of total inhibition at 10 μM as seen by ADAC.