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. Author manuscript; available in PMC: 2012 Jul 1.

Published in final edited form as: Med Res Rev. 2010 Feb 4;31(4):483–519. doi: 10.1002/med.20187

Table VII.

VMAT Inhibition Kinetic Parameters of Tetrabenazine and its Derivatives


Cpd.	Source of VMAT	VMAT Affinity K_dor K _i(nM)	Refs.
5	Chromafin granule memb.	1.3^a	34
78	Rat brain homog.	6^b	82
79	Rat brain homog.	20^b	82
80	Rat brain homog.	3.9^c	77, 78
81	Rat brain homog.	2.6^d	85
82	Rat brain homog.	12^d	85
83	Chromaffin granule memb.	6^c	36
84	Chromaffin granule memb.	110^b	36
85	Rat brain homog.	28^b	145
86	Rat brain homog.	~ 25–30	83
87(+)	Rat brain homog.	0.22^a	81, 84
88(±)	Mouse striatal homog.	0.76^a	86
89(±)	Mouse striatal homog.	0.56^a	86
89(+)	Mouse striatal homog.	0.1±0.01	88
90(+)	Rat striatal homog.	0.08	91

^a

K_d.

^b

K_i for [³H]DTBZOH binding.

^c

IC₅₀ for [³H]DTBZOH binding.

^d

K_i for [³H]MTBZ binding.