Effects of dihydropyridine calcium channel ligands on rat brain gamma-aminobutyric acidB receptors.
This study shows that low nanomolar concentrations of the calcium channel antagonist nifedipine displaced [3H]baclofen labeling of gamma-aminobutyric acidB (GABAB) receptors, whereas similar concentrations of two calcium channel agonists stimulated this GABAB receptor labeling. Neither effect was likely to be due to dihydropyridine (DHP) binding to baclofen recognition sites, because the inhibitory ligand nifedipine primarily affected apparent receptor density rather than affinity. Although these results could reflect the coupling of GABAB receptors with calcium channels, they do not rule out other, possibly more direct interactions between GABAB receptors and DHP binding sites. These DHP effects occur at much lower concentrations and display other significant differences from previously reported effects of DHPs on other transmitter receptors.
Al-Dahan
M I
MI
Department of Cell Biology, Baylor College of Medicine, Houston, TX 77030.
Thalmann
R H
RH
D001498:3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester / Q000494:pharmacology; D000818:Animals; D001418:Baclofen / Q000378:metabolism; D001667:Binding, Competitive; D015220:Calcium Channels / Q000378:metabolism*; D004095:Dihydropyridines / Q000378:metabolism*; D008297:Male; D009543:Nifedipine / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*
D015220:Calcium Channels; D004095:Dihydropyridines; D011963:Receptors, GABA-A; D001498:3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester; C038806:1,4-dihydropyridine; D001418:Baclofen; D009543:Nifedipine