GABAB Receptor Type | CGP7930 | IC50GABA | High-Affinity Component | n |
---|---|---|---|---|
μM | % | |||
Dimer (1b/2) | 0 (control) | 5.2 ± 1.3 | 34 ± 3.1 | 4 |
356 ± 66 | ||||
30 | 1.9 ± 1.0 (4-150) | 27 ± 4.2 | 4 | |
291 ± 91 | ||||
Monomer (1b) | 0 (control) | 121 ± 6 | 3 | |
30 | 111 ± 5 | 3 |
The binding of the antagonist radioligand [3H]CGP62349 to membranes from stably transfected CHO cells was measured in a scintillation proximity assay using WGA coated SPA beads. The displacement of [3H]CGP62349 from heterodimeric receptors by GABA was significantly better fitted by a two-site model, whereas for the GABAB(1b) monomer, the data were adequately fitted by a one-site model (F-test, GraphPad Prism software). The data shown are means ± S.E.M. from n independent experiments.
↵4-150 , p = 0.06 versus the corresponding control value.