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IC50: 5 nM

CGP 55845 is a potent, selective GABAB receptor antagonist that abolishes agonist binding (pKi = 8.35) and blocks GABA and glutamate release (pEC50 values are 8.08 and 7.85 respectively). CGP 55845 prevents GABAB responses to baclofen (IC50 = 130 nM in an isoproterenol assay) and increases the hypoglycemic response to glucose in vitro. [1,2]

Presynaptic GABAB receptors seem to regulate the release of several neurotransmitters. Baclofen, the GABAB agonist, that prevents the release of GABA itself via autoreceptors, was 10 times more potent in antagonizing the inhibitory effect of (-)-baclofen on the release of GABA and of somatostatin-like immunoreactivity (SRIF-LI) than of glutamate. However, CGP 35348 was about 70 times more potent in preventing the effect of baclofen on glutamate and SRIF-LI than on GABA release.

In vitro: Antagonist CGP 55845A of the GABAB receptor in the presence of CNQX and d(2)-2-amino-5-phosphonovaleric acid prevented the inhibitory postsynaptic potential-B and paired-pulse depression. [3].

This secretion was cadmium sensitive, potentiated by CGP 55845, and blocked by ketanserin. Taken together these data suggest that CB receptors act as direct glucosensors, and that processing of hypoglycaemia utilizes similar neurotransmitter and neuromodulatory mechanisms as hypoxia [4]. The convulsant 4-aminopyridine (4-AP) and the GABAB receptor antagonist CGP 55845 both applied to adult guinea pig hippocampal to slices, resulting in eliciting giant GABA-mediated postsynaptic potentials (GPSPs) and epileptiform discharges. [5].

In vivo: So far, no study in vivo has been conducted.

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