. 2011 Mar;336(3):940–951. doi: 10.1124/jpet.110.175117

TABLE 1.

Affinity values (K_i) of MTD analogs, lobeline, MTD, and standard compounds for nicotinic receptors, DAT, SERT, and VMAT2 binding and function

Compound	[³H]Nicotine Binding K_i ± S.E.M.	[³H]MLA Binding K_i ± S.E.M.	DAT [³H]DA Uptake K_i ± S.E.M.	SERT [³H]5-HT Uptake K_i ± S.E.M.	VMAT2 [³H]DTBZ Binding K_i ± S.E.M.	VMAT2 [³H]DA Uptake K_i ± S.E.M.
			μM
Nicotine	0.003 ± 0.0002^a	0.37 ± 0.08^a	N.D.	N.D.	N.D.	N.D.
GBR 12909	N.D.	N.D.	0.00097 ± 0.0001^a	N.D.	N.D.	N.D.
Fluoxetine	N.D.	N.D.	N.D.	0.0065 ± 0.0001^a	N.D.	N.D.
Ro-4-1284	N.D.	N.D.	N.D.	N.D.	0.028 ± 0.003^a	0.018 ± 0.002^a
Lobeline	0.004 ± 0.0001	6.26 ± 1.30	28.2 ± 6.73	46.8 ± 3.70	2.04 ± 0.26^b	1.27 ± 0.46
MTD	>100^c	>100^c	0.10 ± 0.01	7.00 ± 1.30	9.88 ± 2.22^b	0.46 ± 0.11
UKMH-101	>100	>100	11.5 ± 1.90	0.71 ± 0.09	31.8 ± 5.84	0.88 ± 0.19
UKMH-102	>100	>100	25.1 ± 2.93	1.37 ± 0.09	12.3 ± 4.70	0.22 ± 0.05
UKMH-103	>100	>100	16.2 ± 1.20	2.10 ± 0.51	20.3 ± 3.73	0.79 ± 0.18
UKMH-104	>100	>100	5.25 ± 0.46	2.67 ± 0.51	15.0 ± 5.22	0.88 ± 0.26
UKMH-105	>100	>100	6.27 ± 0.60	18.3 ± 7.50	4.60 ± 1.70	0.22 ± 0.01
UKMH-106	>100	>100	6.90 ± 1.10	20.7 ± 4.90	41.3 ± 14.3	0.32 ± 0.12
UKMH-107	>100	>100	68.2 ± 6.93	0.51 ± 0.05	7.27 ± 2.28	1.03 ± 0.19
UKMH-108	>100	>100	39.0 ± 16.3	0.61 ± 0.08	3.42 ± 0.26	0.33 ± 0.08
UKMH-109	>100	>100	>100	16.3 ± 4.10	91.3 ± 26.2	2.27 ± 1.13
UKMH-110	>100	>100	58.1 ± 18.7	13.4 ± 4.10	10.4 ± 2.62	0.36 ± 0.12
UKMH-111	>100	>100	>100	16.1 ± 2.91	32.6 ± 6.79	3.82 ± 1.99
UKMH-112	>100	>100	5.50 ± 0.26	0.71 ± 0.19	15.5 ± 1.61	0.58 ± 0.08

N.D., not determined. UKMH-110, (3Z,5Z)-1-methyl-3,5-bis(thiophen-3-ylmethylene)piperidine; UKMH-111, (3Z,5Z)-3,5-bis(furan-2-ylmethylene)-1-methylpiperidine.

n = 3–4 rats.

Data taken from Zheng et al., 2005.

Data taken from Miller et al., 2001.