Table 1.

Inhibition constants (K_i) for GZ-793A (3) analogs at the [³H]DTBZ binding site and [³H]-DA uptake site on VMAT2

Comp	R	[3H]DTBZ Bindinga	VMAT2 [3H]DA uptakec
		Ki±SEM (μM)b	Ki±SEM (nM)
3	-	8.29 ± 2.79	29 ± 8
11a	H	5.91 ± 1.57	279 ± 35
11b	2-OCH3	2.35 ± 0.44	270 ± 6
11c	3-OCH3	2.28 ± 0.44	160 ± 10
11d	4-OCH3	3.94 ± 1.12	49 ± 9
11e	3-F	6.76 ± 1.68	170 ± 15
11f	4-OCHF2	0.56 ± 0.23	45± 7
11g	3,4-methylenedioxy	8.47 ± 5.19	269 ± 28
11h	3,4-dimethoxy	> 100	3780 ± 230
11i	3,5-difluoro	4.06 ± 0.81	200 ± 1

^aAll binding experiments have n=3,

^bEach K_i value represents mean ±SEM.

^cAll uptake experiments represent n=4