GABA and the GABAB receptor agonist baclofen activated a potassium conductance in acutely dissociated hippocampal CA3 neurons. Baclofen-activated current required internal GTP, was purely potassium selective, and showed strong inward rectification. As with acetylcholine-activated current in atrial myocytes, external Cs+ blocked inward but not outward current in a highly voltage-dependent manner...

The compounds CGP7930 [2,6-Di-tert-butyl-4-(3-hydroxy-2,2dimethyl-propyl)-phenol] and its close analog CGP13501 were identified as positive modulators of -aminobutyric acidB (GABAB) receptor function. They potentiate GABA-stimulated guanosine 5 -O-(3-[S]thiotriphosphate) (GTP [S]) binding to membranes from a GABAB(1b/2) expressing Chinese hamster ovary (CHO) cell line at low micromolar concentr...

N,N -Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6diamine (GS39783) and structurally related compounds are described as novel allosteric enhancers of GABAB receptor function. They potentiate GABA-stimulated guanosine 5 -O-(3-[S]thio)triphosphate ([S]GTP S) binding to membranes from a GABAB(1b/2)-expressing Chinese hamster ovary cell line at low micromolar concentrations, but do not stim...

We used standard techniques of receptor autoradiography to study the distribution of inhibitory and excitatory amino acid neurotransmitter receptors in human normal cerebellar cortex. Benzodiazepine (BDZ) receptor density was relatively high in both granule cell and molecular layers. GABAA receptor density was highest in granule cell layer with lower receptor density in molecular layer. There w...

Synchronized network responses in thalamus depend on phasic inhibition originating in the thalamic reticular nucleus (nRt) and are mediated by the neurotransmitter g-aminobutyric acid (GABA). A suggested role for intra-nRt connectivity in inhibitory phasing remains controversial. Recently, functional GABA type B (GABAB) receptors were demonstrated on nRt cells, and the slow time course of the G...

PCPGABA, injected into the cisterna magna, significantly stimulated gastric acid secretion in the perfused rat stomach preparation. This secretagogue action was dose-dependent (0.5-2 micrograms/rat). The peak response occurred within 60 min and lasted up to 100 min. The secretagogue action by PCPGABA was completely reduced by truncal vagotomy. Intracisternal injection of 5-aminovaleric acid, a ...

1508-1517, 1998. Whole cell recordings (nystatin-perforated patch) were carried out on magnocellular neurons of the rat supraoptic nucleus (SON) to study the modulation of inhibitory postsynaptic currents (IPSCs) by gamma-aminobutyric acid-B (GABAB) receptors. Field stimulation adjacent to the SON in the presence of kynurenic acid, evoked monosynaptic GABAergic IPSCs. Baclofen reversibly reduce...