. Author manuscript; available in PMC: 2010 Jan 8.

Published in final edited form as: J Med Chem. 2009 Jan 8;52(1):62–73. doi: 10.1021/jm800817h

Table 1.

Binding Affinities (Ki (nM)) of Candidate NET Ligands in in vitro Competition Assays with Human Monoamine Transporters^a and Lipophilicities (log P_7.4)

compound	K_i for NET^b	K_i for SERT^c	K_i for DAT^d	NET selectivity		log P_7.4
				SERT/NET	DAT/NET
MENET, 1	1.02 ± 0.11	93 ± 20	327 ± 39	92	321	2.04
FENET, 2	3.14 ± 0.17	430 ± 14	>6000	137	>2000	2.00
FPNET, 3	3.68 ± 0.92	463 ± 24	>6000	126	>2000	2.29
MESNET, 4	0.30 ± 0.03	14.80 ± 2.83	275 ± 83	49	917	2.47
(S,S)-reboxetine	1.04 ± 0.16	661 ± 36	>2000	636	>2000
(S,S)-MeNER	0.95 ± 0.03	185 ± 3	>2000	195	>2000

All K_i values are reported as nanomolar (nM) values. The data are expressed as geometric mean ± standard deviation of at least three separate experiments performed in triplicate.

Competitive binding vs [³H]nisoxetine in HEK-293 cells transfected with human norepinephrine transporters.

Competitive binding vs [³H]citalopram in HEK-293 cells transfected with human serotonin transporters.

Competitive binding vs [¹²⁵I]RTI-55 in canine kidney cells transfected with human dopamie transporters.