TABLE 1.
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.
n = 3–4 rats.
Data for [3H]DTBZ binding for lobeline and lobelane taken from Nickell et al., 2010.