. Author manuscript; available in PMC: 2008 Dec 8.

Published in final edited form as: J Med Chem. 2005 Dec 29;48(26):8103–8107. doi: 10.1021/jm050726b

Table 1.

Potency of adenosine derivatives at human A₁, A_2A, and A₃ARs and the rat A₃AR _a and maximal agonist effects at human A₃ARs expressed in CHO cells.^a


No.	N⁶-R′	C2-R	K_i (hA₁AR) nM^a	K_i (hA_2AAR) nM^a	K_i (hA₃AR) nM^a	% Activation (hA₃AR)^b at 10 μM	K_i (rA₃AR)
1^c	CP	H	34.1 ± 6.1	6420 ± 630	13.1 ± 5.1	93 ± 7	10.2 ± 2.1
2^c	CP	Cl	18.3 ± 6.3^g	3250 ± 300	3.7 ± 0.9	101 ± 10	5.8 ± 1.6
3^c	NB	Cl	190 ± 37	>10,000	14.6 ± 3.2	92 ± 6	9.6 ± 2.7
4^d	CP	H	0.45±0.04^b	462	240±36	72±12	97±4
5^d	CP	Cl	0.83^e	2270^e	38 ± 6	0	237±71^f
6^d	NB	H	0.48±0.01	>10,000	229±76	112±25	103±1

All AR experiments were performed using adherent CHO cells stably transfected with cDNA encoding the human or rat ARs. Percent activation of the human A₃AR was determined at 10 μM. Binding at human A₁ and A_2AARs in this study was carried out as described in Methods using [³H]R-PIA or [³H]CGS 21680 as a radioligand. Values from the present study are expressed as mean ± s.e.m., n = 3–5.

Percent activity at 10 μM, relative to 10 μM Cl-IB-MECA (A₃).

1, MRS3706; 2, MRS3630; 3, MRS3638.

Data from Gao et al., unless noted.²²,²³

Data from Klotz et al.²⁸

Data from van Galen et al.²⁹

K_i at rat A₁ AR is 17.4 ± 2.7 nM.

ND not determined. CP, cyclopentyl; NB, 7-norbornyl.