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. 2011 Oct;339(1):286–297. doi: 10.1124/jpet.111.184770

TABLE 1.

Summary for standards, lobeline, lobelane, and N-1,2-diol analogs

Compound Ki ± S.E.M.
DAT, [3H]DA Uptake SERT, [3H]5-HT Uptake VMAT2, [3H]DTBZ Binding VMAT2, [3H]DA Uptake
μM
Standards
    GBR 12909 0.0009 ± 0.0001a N.D. N.D. N.D.
    Cocaine 0.48 ± 0.07 N.D. N.D. N.D.
    Fluoxetine N.D. 0.007 ± 0.0001a N.D. N.D.
    Ro-4-1284 0.04 ± 0.005 0.02 ± 0.003 0.03 ± 0.003a 0.02 ± 0.002a
Lobeline, lobelane, and N-1,2-diol analogs
    Lobeline 28.2 ± 6.73 46.8 ± 3.70 2.04 ± 0.64b 1.27 ± 0.46
    Lobelane 1.05 ± 0.03 3.60 ± 0.35 0.97 ± 0.19b 0.067 ± 0.007
    GZ-745A 0.60 ± 0.06 8.43 ± 2.80 0.56 ± 0.08 0.19 ± 0.05
    GZ-745B 1.08 ± 0.12 11.0 ± 3.12 1.28 ± 0.13 0.86 ± 0.12
N-1,2-Diol analogs containing 1-naphthyl or 4-biphenyl substituents
    GZ-794A 1.43 ± 0.14 0.31 ± 0.08 0.31 ± 0.07 0.033 ± 0.002
    GZ-794B 1.57 ± 0.16 0.16 ± 0.04 0.13 ± 0.01 0.08 ± 0.01
    GZ-796A 8.33 ± 1.46 5.30 ± 0.96 >100 0.79 ± 0.23
    GZ-796B 3.43 ± 0.63 2.55 ± 0.77 90.2 ± 9.70 2.25 ± 1.30
N-1,2-Diol analogs containing aromatic methoxy or methylene-dioxy substituents
    GZ-790A 3.80 ± 0.69 3.14 ± 1.18 0.46 ± 0.22 0.14 ± 0.02
    GZ-790B 6.67 ± 2.15 8.03 ± 2.30 2.73 ± 0.68 0.52 ± 0.04
    GZ-792A 2.90 ± 0.23 1.33 ± 0.46 1.04 ± 0.73 0.49 ± 0.06
    GZ-792B 4.77 ± 1.03 0.94 ± 0.14 1.87 ± 0.69 0.79 ± 0.08
    GZ-793A 1.44 ± 0.27 9.36 ± 2.74 8.29 ± 2.79 0.029 ± 0.008
    GZ-793B 3.40 ± 0.82 10.4 ± 2.75 7.74 ± 2.34 0.18 ± 0.04
    GZ-797A 2.46 ± 0.16 2.10 ± 0.70 1.30 ± 0.05 0.16 ± 0.04
    GZ-797B 2.21 ± 0.31 2.63 ± 0.60 5.61 ± 0.62 0.76 ± 0.04
N-1,2-Diol analogs containing aromatic halogeno substituents
    GZ-791A 0.25 ± 0.07 1.32 ± 0.46 1.00 ± 0.16 0.19 ± 0.06
    GZ-791B 0.62 ± 0.05 2.87 ± 0.50 1.08 ± 0.38 1.03 ± 0.16
    GZ-795A 3.87 ± 0.89 2.15 ± 0.38 10.4 ± 0.65 0.14 ± 0.04
    GZ-795B 9.50 ± 2.53 1.86 ± 0.39 13.9 ± 0.38 0.09 ± 0.04

N.D., not determined.

a

n = 3–4 rats.

b

Data for [3H]DTBZ binding for lobeline and lobelane taken from Nickell et al., 2010.