. Author manuscript; available in PMC: 2010 Dec 21.

Published in final edited form as: Bioconjug Chem. 2009 Sep 28;20(10):1888–1898. doi: 10.1021/bc9001689

Table 2.

Binding and functional assay results of monomers and dendrimers at four subtypes of hARs.^a

cmpd	binding^b at ARs						activation^c at ARs
	hA₁		hA_2A		hA₃		hA_2A		hA_2B
	K_i [nM]	% inhibition	K_i [nM]	% inhibition	K_i [nM]	% inhibition	EC₅₀ [nM]	% activation	% activation
1	5780 ± 590	24.9 ± 4.6	67 ± 19	84.7 ± 0.9	247 ± 79	59.8 ± 4.4	53.0 ± 16.0	100 ± 10	3.6 ± 6.3
2	168 ± 36	56.9 ± 9.1	12 ± 6	101 ± 1	38 ± 11	85.3 ± 3.2	8.2 ± 1.7	96.0 ± 6.0	5.5 ± 4.7
3	984 ± 223	36.9 ± 7.5	210 ± 19	82.1 ± 0.3	58 ± 24	85.2 ± 11.4	51.0 ± 8.0	103 ± 5	-1.7 ± 5.0
7a	n.d.^d	5.5 ± 8.8	n.d.^d	1.6 ± 7.4	n.d.^d	-13.4 ± 2.7	n.d.^d	2.4 ± 1.7	5.3 ± 8.9
7b	n.d.^d	13.8 ± 4.5	n.d.^d	-11.6 ± 2.5	n.d.^d	-17.2 ± 5.2	n.d.^d	n.a.^d	1.6 ± 7.3
7d	n.d.^d	7.1 ± 4.5	n.d.^d	3.2 ± 4.9	n.d.^d	-7.5 ± 2.2	n.d.^d	n.a.^d	-4.4 ± 3.8
9a	n.d.^d	12.2 ± 1.6	488 ± 59	61.4 ± 2.0	n.d.^d	24.4 ± 6.5	n.d.^d	92.6 ± 5.4	1.4 ± 5.5
9b	n.d.^d	19.3 ± 3.6	496 ± 18	62.7 ± 1.2	n.d.^d	27.6 ± 3.2	n.d.^d	101 ± 5	16.6 ± 3.7
9d	n.d.^d	13.3 ± 3.1	752 ± 34	55.8 ± 1.8	n.d.^d	25.4 ± 4.0	n.d.^d	91.0 ± 8.3	9.4 ± 5.4
10c	4870 ± 1360	19.9 ± 4.8	151 ± 36	81.2 ± 1.5	1130 ± 310	29.0 ± 12.0	11.2 ± 4.9	90.0 ± 6.7	2.8 ± 1.4
10d	4230 ± 1310	19.8 ± 2.6	215 ± 12	75.5 ± 3.1	1320^e	24.4 ± 8.0	60.6 ± 12.8	97.0 ± 7.1	3.3 ± 3.0

Values are presented as the mean ± standard error of three or more independent experiments. The hA₁, hA_2B, and hA₃ ARs were expressed in CHO cells and the hA_2A AR in HEK-293 cells for binding and in CHO cells for the functional assay.

K_i values were determined through the radioligand binding, and the percent inhibition refers to the inhibition of binding at 1 μM.

EC₅₀ values were determined by measuring the degree of stimulation of adenylate cyclase in cells stably expressing hA_2A or hA_2B AR. Percent activation refers to the activation of adenylate cyclase in comparison to the effects exerted by the full agonist NECA (100%) at 10 μM.

n.d. = not determined, i.e., binding/functional experiment was not conducted, or n.a. = no binding/activation was detected under the given assay conditions.

Performed only once.