. Author manuscript; available in PMC: 2021 Nov 22.

Published in final edited form as: Biochem Pharmacol. 2003 Feb 15;65(4):525–534. doi: 10.1016/s0006-2952(02)01556-3

Table 1.

Dissociation rates (k₋₁) of radiolabeled agonists and antagonists in the absence or presence of amiloride analogues

Derivative	k₋₁ (min⁻¹)
	A₁ receptor		A_2A receptor		A₃ receptor
	[³H]R-PIA (agonist)	[³H]DPCPX (antagonist)	[³H]CGS21680 (agonist)	[³H]ZM241385^a (antagonist)	[¹²⁵I]I-AB-MECA (agonist)	[³H]PSB-11 (antagonist)
Control	0.012 ± 0.003	0.13 ± 0.02	0.066 ± 0.009	0.007 ± 0.002	0.059 ± 0.009	0.007 ± 0.001
+Amiloride (1 mM)	0.012 ± 0.002	0.19 ± 0.02^*	0.087 ± 0.022	0.008 ± 0.002	0.058 ± 0.006	0.008 ± 0.002
+DMA (0.1 mM)	0.013 ± 0.003	0.25 ± 0.04^*	0.084 ± 0.017	ND^b	0.047 ± 0.009^*	0.009 ± 0.001^*
+HMA (0.1 mM)	0.013 ± 0.003	0.22 ± 0.02^*	ND	0.080 ± 0 010^*	0.031 ± 0.006^*	0.016 ± 0 003^*
+MIBA(0.1mM)	ND	ND	ND	0.040 ± 0005^*	0.035 ± 0.007^*	0.011 ±0002^*

Human A₃ receptors were expressed in CHO cells, and the rat A₃ receptor of RBL-2H3 cells was used. A₁ and A_2A receptors of rat brain (forebrain and striatum, respectively) were used. The k₋₁ values for [³H]PSB-11 were from an experiment performed at 4°; similar results from an experiment performed at 25° are shown in Fig. 4A. Results are expressed as mean ± SEM and are from at least three independent experiments performed in duplicate.

Data from Ref. [19].

ND = not determined.

P < 0.05, compared with the control.