R | Compound | IC50 | Imax | Reference |
---|---|---|---|---|
nM | % | |||
-H | 1 | 51 | 95 | a,b |
-CH3 | 2 | 80 | 94 | a,b |
-CH2CH3 | 3 | 260 | 69 | 1-b |
-CHCH2 | 4 | 120 | 94 | 1-b |
-CCH | 5 | 64 | 93 | 1-b |
-CC-C4H9 | 6 | 80 ± 12 | 90 ± 2 | |
-CC-C6H5 | 7 1-c | 21 ± 3 | 33.2 ± 0.4 | |
3700 ± 600 | 55 ± 4 |
IC50 and Imax values for inhibition of 2 nM [35S]TBPS binding to rat brain cortical membranes in the presence of 5 μM GABA. Values are mean ± S.E. of at least three independent experiments. Hill slope values were 1.0 for all one-component compounds.