. Author manuscript; available in PMC: 2011 May 9.

Published in final edited form as: J Pharmacol Exp Ther. 2008 May 6;326(2):563–576. doi: 10.1124/jpet.108.136630

TABLE 2.

Summary of inhibitory activities of N,N′-alkane-diyl-bis-3-picolinium analogs (bAPi) in [³H]nicotine and [³H]MLA binding assays, [³H]DA overflow assay and [³H]DA uptake assay.

Compound	[³H]Nicotine Binding Assay K_i (μM)	[³H]MLA Binding Assay K_i (μM)	[³H]DA Overflow Assay		[³H]DA Uptake Assay K_i (μM)
Compound	[³H]Nicotine Binding Assay K_i (μM)	[³H]MLA Binding Assay K_i (μM)	IC₅₀ (μM)	Imax (%)	[³H]DA Uptake Assay K_i (μM)

bPiHxI (C₆)	>100^a	>100	>100	-	>100
bPiHpB (C₇)	>100	>100	0.06 ± 0.03	54 ± 5
bPiOI (C₈)	>100	>100	0.30 ± 0.18	57 ± 9	>100
bPiNB (C₉)	79.9 ± 16.6	>100	5.81 ± 5.07	61 ± 11	>100
bPiDI (C₁₀)	>100	>100	0.18 ± 0.11	60 ± 9	>100
bPiUB (C₁₁)	69.2 ± 28.9	>100	1.12 ± 0.65	62 ± 6	>100
bPiDDB (C₁₂)	48.6 ± 17.2	>100	0.002 ± 0.001	64 ± 4	>100

Data are mean ± S.E.M.; n = 5–10 rats/analog for [³H]DA overflow assay; n = 3–5 rats/analog for binding and uptake assays.