TABLE 1

Effects of CsA on Brain Uptake of Radioactivity After Injection of Each Radioligand into Mice

	Brain uptake of radioligand			Brain-to-blood ratio
Radioligand	Control (%ID/g)	Treatment (%ID/g)	Ratio	Control	Treatment	Ratio
In this study
¹¹C-Verapamil	0.40 ± 0.04	4.44 ± 0.52^*	11.05	0.50 ± 0.08	4.35 ± 0.66^*	8.76
¹¹C-TMSX	1.92 ± 0.17^‡	3.24 ± 0.38^*	1.69	1.29 ± 0.13	2.04 ± 0.32^*	1.59
¹¹C-MPDX	1.87 ± 0.26	3.67 ± 0.84^†	1.96	0.79 ± 0.11	1.47 ± 0.43^†	1.86
¹¹C-PK11195	1.05 ± 0.05	1.71 ± 0.62	1.33	2.07 ± 0.36	1.56 ± 0.92	0.86
¹¹C-Flumazenil	2.25 ± 0.27	7.54 ± 1.09^*	3.35	2.94 ± 0.53	4.62 ± 0.65^†	1.57
¹¹C-Raclopride	1.16 ± 0.17^¶	1.70 ± 0.28^†	1.46	1.50 ± 0.20	1.16 ± 0.36	0.77
¹¹C-Pyrilamine	2.71 ± 0.18	4.61 ± 0.42^*	1.70	7.07 ± 0.78	3.21 ± 0.30^*	0.46
¹¹C-PIB	0.56 ± 0.07	0.75 ± 0.11	1.34	0.56 ± 0.09	0.34 ± 0.06	0.61
¹¹C-Donepezil	1.91 ± 0.20	6.13 ± 1.07^*	3.21	4.60 ± 0.44	10.93 ± 2.34^*	2.38
Previously reported^§
¹¹C-Carazolol (14)	0.12 ± 0.03	0.62 ± 0.05	5.17	1.50	2.50	1.67
¹⁸F-Fluorocarazolol (14)	0.77 ± 0.19	1.82 ± 0.22	2.34	2.75	5.87	2.13
¹⁸F-MPPF (15)	0.22	1.15	5.23	1.47	2.41	1.64
¹¹C-SA4503 (16)	3.96 ± 0.20	3.84 ± 0.55	0.99	4.19 ± 0.73	4.33 ± 0.80	1.03
¹¹C-GR218231 (17)	0.21 ± 0.05	2.85 ± 0.56	13.6	0.22	2.50	11.4

↵* P < 0.001 (Student t test, compared with control).
↵† P < 0.01 (Student t test, compared with control).
↵‡ %ID/g in striatum rich in corresponding receptors was 4.99 ± 0.46.
↵¶ %ID/g in striatum rich in corresponding receptors was 5.30 ± 0.72.
↵§ Data are quoted or recalculated from the original reports, where assay 1 was performed on rats and levels of radioactivity in frontal cortex (14), hippocampus (15), whole brain (16), or neocortex (17) and plasma, instead of blood, were expressed as standardized uptake value: (radioactivity of tissue/gram of tissue)/(total injected radioactivity/gram of whole-body weight). Significant modulation by CsA was reported for 4 radioligands but not ¹¹C-SA4503.
Data are mean ± SD (n = 4–6).