Potent, selective GABAB
receptor antagonist (IC50
= 5 nM) that prevents agonist binding (pKi
= 8.35) and inhibits GABA and glutamate release (pEC50
values are 8.08 and 7.85 respectively). Inhibits GABAB
responses to baclofen (IC50
= 130 nM in an isoproterenol assay) and potentiates the hypoglycemic response to glucose in vitro
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Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain.
Cunninghan and Enna
Brain Res., 1996;720:220
The GABAB antagonist CGP 55845A reduces presynaptic GABA1 actions in neurons of the rat in vitro.
Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices.
Salah and Perkins
GABA and glutamate release affected by GABAB receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors.
Waldmeier et al.
Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body.
Zhang et al.
Potent, orally active GABAB receptor antagonists.
Froestl et al.
The citations listed below are publications that use Tocris products. Selected citations for CGP 55845 hydrochloride include:
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