CGP 55845 hydrochloride
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.
Sold with the permission of Novartis Pharma AG
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||43.87||100 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 438.71. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.28 mL||11.4 mL||22.79 mL|
|5 mM||0.46 mL||2.28 mL||4.56 mL|
|10 mM||0.23 mL||1.14 mL||2.28 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References are publications that support the biological activity of the product.
Cunninghan and Enna (1996) Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain. Brain Res. 720 220 PMID: 8782915
Deisz (1999) The GABAB antagonist CGP 55845A reduces presynaptic GABA1 actions in neurons of the rat in vitro. Neuroscience 93 1241 PMID: 10501448
Salah and Perkins (2008) Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology 55 47 PMID: 18538357
Waldmeier et al (1994) GABA and glutamate release affected by GABAB receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors. Br.J.Pharmacol. 113 1515 PMID: 7889310
Zhang et al (2007) Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. J.Physiol. 578 735 PMID: 17124268
Froestl et al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8 127
If you know of a relevant reference for CGP 55845 hydrochloride, please let us know.
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Keywords: CGP 55845 hydrochloride, CGP 55845 hydrochloride supplier, Potent, selective, GABAB, antagonists, Receptors, CGP55845, hydrochloride, 1248, Tocris Bioscience
87 Citations for CGP 55845 hydrochloride
Citations are publications that use Tocris products. Selected citations for CGP 55845 hydrochloride include:
Brodnik et al (2018) Local GABAA receptor mediated suppression of dopamine release within the nucleus accumbens. ACS Chem Neurosci PMID: 30253088
Meira et al (2018) A hippocampal circuit linking dorsal CA2 to ventral CA1 critical for social memory dynamics. Nat.Commun. 9 4163 PMID: 30301899
Zhu et al (2011) Suppression of PKR promotes network excitability and enhanced cognition by interferon-γ-mediated disinhibition. Cell 147 1384 PMID: 22153080
Zschenderlein et al (2011) Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1. PLoS One 6 e16116 PMID: 21249195
Straub et al (2011) Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1. Nat Neurosci 14 866 PMID: 21623363
Wei et al (2011) Diffuse and specific tectopulvinar terminals in the tree shrew: synapses, synapsins, and synaptic potentials. PLoS One 6 e23781 PMID: 21858222
Hays et al (2011) Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry. J Neurosci 31 14223 PMID: 21976507
Dilger et al (2011) Requirements for synaptically evoked plateau potentials in relay cells of the dorsal lateral geniculate nucleus of the mouse. J Physiol 589 919 PMID: 21173075
Allen et al (2011) The SK2-long isoform directs synaptic localization and function of SK2-containing channels. Nat Neurosci 14 744 PMID: 21602822
Karson et al (2008) Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others. Biomed Res Int 54 117 PMID: 17689570
Molineux et al (2008) Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons. J Neurosci 100 2684 PMID: 18768644
Hirono (2017) Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells. Neuropharmacology 118 79 PMID: 28300552
Tabatadze et al (2015) Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus. J Neurosci 35 11252 PMID: 26269634
Medrihan et al (2015) Asynchronous GABA Release Is a Key Determinant of Tonic Inhibition and Controls Neuronal Excitability: A Study in the Synapsin II-/- Mouse. Cereb Cortex 25 3356 PMID: 24962993
Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 Dopamine Autoreceptor-Mediated Neurotransmission in Midbrain Dopaminergic Neurons. J Neurosci 35 11144 PMID: 26245975
Dilger et al (2015) Absence of plateau potentials in dLGN cells leads to a breakdown in retinogeniculate refinement. J Neurosci 35 3652 PMID: 25716863
Yang et al (2015) Non-additive modulation of synaptic transmission by serotonin, adenosine, and cholinergic modulators in the sensory thalamus. Front Cell Neurosci 9 60 PMID: 25852468
Muralidhar et al (2014) Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex. Front Neuroanat 7 52 PMID: 24474905
Kramer et al (2014) Inhibitory glycinergic neurotransmission in the mammalian auditory brainstem upon prolonged stimulation: short-term plasticity and synaptic reliability. Front Neural Circuits 8 14 PMID: 24653676
Marcott et al (2014) Phasic dopamine release drives rapid activation of striatal D2-receptors. Neuron 84 164 PMID: 25242218
Qi et al (2014) Longitudinal testing of hippocampal plasticity reveals the onset and maintenance of endogenous human Aβ-induced synaptic dysfunction in individual freely behaving pre-plaque transgenic rats: rapid reversal by anti-Aβ agents. Acta Neuropathol Commun 2 175 PMID: 25540024
Toader et al (2013) Dentate gyrus network dysfunctions precede the symptomatic phase in a genetic mouse model of seizures. Nat Commun 7 138 PMID: 24009558
Medrihan et al (2013) Synapsin II desynchronizes neurotransmitter release at inhibitory synapses by interacting with presynaptic calcium channels. Proc Natl Acad Sci U S A 4 1512 PMID: 23443540
Shen et al (2008) Dichotomous dopaminergic control of striatal synaptic plasticity. Science 321 848 PMID: 18687967
Jüngling et al (2008) Neuropeptide S-mediated control of fear expression and extinction: role of intercalated GABAergic neurons in the amygdala. Neuron 59 298 PMID: 18667157
Atherton et al (2008) Autonomous initiation and propagation of action potentials in neurons of the subthalamic nucleus. J Physiol 586 5679 PMID: 18832425
Maher and Westbrook (2008) Co-transmission of dopamine and GABA in periglomerular cells. J Neurosci 99 1559 PMID: 18216231
Darbin and Wichmann (2008) Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys. J Neurophysiol 99 1294 PMID: 18216224
Chiu and Castillo (2008) Input-specific plasticity at excitatory synapses mediated by endocannabinoids in the dentate gyrus. Neuropharmacology 54 68 PMID: 17706254
Power and Sah (2008) Competition between calcium-activated K+ channels determines cholinergic action on firing properties of basolateral amygdala projection neurons. J Neurosci 28 3209 PMID: 18354024
Wu et al (2008) Coupling of L-type Ca2+ channels to KV7/KCNQ channels creates a novel, activity-dependent, homeostatic intrinsic plasticity. J Neurophysiol 100 1897 PMID: 18715900
McElligott (2008) Alpha1-adrenergic receptor-induced heterosynaptic long-term depression in the bed nucleus of the stria terminalis is disrupted in mouse models of affective disorders. Neuropsychopharmacology 33 2313 PMID: 18046308
Engbers et al (2012) Intermediate conductance calcium-activated potassium channels modulate summation of parallel fiber input in cerebellar Purkinje cells. J Neurosci 109 2601 PMID: 22308379
Zhu et al (2012) Persistent inflammation increases GABA-induced depolarization of rat cutaneous dorsal root ganglion neurons in vitro. Neurobiol Dis 220 330 PMID: 22728089
Allen et al (2011) SK2 channels are neuroprotective for ischemia-induced neuronal cell death. Neuroscience 31 2302 PMID: 21712833
Fukunaga et al (2007) Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices. Br J Pharmacol 151 870 PMID: 17502847
Philippart et al (2016) Differential Somatic Ca2+ Channel Profile in Midbrain Dopaminergic Neurons The Journal of Neuroscience 6 7234 PMID: 27383597
Wozniak et al (2016) Involvement of GABAB Receptor Signaling in Antipsychotic-like Action of the Novel Orthosteric Agonist of the mGlu4 Receptor, LSP4-2022 Current Neuropharmacology 14 413 PMID: 26769224
Dennis et al (2016) Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus. J Neurophysiol 26 414 PMID: 26472558
Delaney and Crane (2016) Presynaptic GABAB receptors reduce transmission at parabrachial synapses in the lateral central amygdala by inhibiting N-type calcium channels. Sci Rep 6 19255 PMID: 26755335
Stratton et al (2014) Embryonic GABA(B) receptor blockade alters cell migration, adult hypothalamic structure, and anxiety- and depression-like behaviors sex specifically in mice. PLoS One 9 e106015 PMID: 25162235
Kallupi et al (2014) Nociceptin/orphanin FQ decreases glutamate transmission and blocks ethanol-induced effects in the central amygdala of naive and ethanol-dependent rats. Neuropsychopharmacology 39 1081 PMID: 24169802
Rio et al (2010) M3 muscarinic acetylcholine receptor expression confers differential cholinergic modulation to neurochemically distinct hippocampal basket cell subtypes. Front Pharmacol 30 6011 PMID: 20427660
Bonislawski et al (2007) Brain injury impairs dentate gyrus inhibitory efficacy. J Neurophysiol 25 163 PMID: 17045484
Takayasu et al (2006) Glial glutamate transporters maintain one-to-one relationship at the climbing fiber-Purkinje cell synapse by preventing glutamate spillover. Mol Pain 26 6563 PMID: 16775144
Selten et al (2016) Increased GABAB receptor signaling in a rat model for schizophrenia Scientific Reports 6 34240 PMID: 27687783
Di Castro et al (2016) The chemokine CXCL16 modulates neurotransmitter release in hippocampal CA1 area Scientific Reports 6 34633 PMID: 27721466
Jung Kim et al (2016) Vasculo-neuronal coupling: retrograde vascular communication to brain neurons The Journal of Neuroscience 14 12624 PMID: 27821575
Mamaligas et al (2016) Nicotinic and opioid receptor regulation of striatal dopamine D2-receptor mediated transmission Scientific Reports 6 37834 PMID: 27886263
Abdi et al (2015) Prototypic and arkypallidal neurons in the dopamine-intact external globus pallidus. Elife 35 6667 PMID: 25926446
Gantz et al (2015) Distinct regulation of dopamine D2S and D2L autoreceptor signaling by calcium. PLoS One 4 PMID: 26308580
Wang et al (2015) Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice. J Neurophysiol 10 e0139332 PMID: 26418566
Bajo et al (2015) IL-1 interacts with ethanol effects on GABAergic transmission in the mouse central amygdala. Am J Physiol Gastrointest Liver Physiol 6 49 PMID: 25852553
Wu et al (2013) Ovarian hormone loss impairs excitatory synaptic transmission at hippocampal CA3-CA1 synapses. J Neurosci 33 16158 PMID: 24107948
Lee et al (2013) TRPM2 channels are required for NMDA-induced burst firing and contribute to H(2)O(2)-dependent modulation in substantia nigra pars reticulata GABAergic neurons. J Neurosci 33 1157 PMID: 23325252
Navarrete et al (2012) Astrocytes mediate in vivo cholinergic-induced synaptic plasticity. PLoS Biol 10 e1001259 PMID: 22347811
Jurgens et al (2012) Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus. PLoS One 7 e45717 PMID: 23029198
Lemos et al (2012) Repeated stress dysregulates κ-opioid receptor signaling in the dorsal raphe through a p38α MAPK-dependent mechanism. J Neurosci 32 12325 PMID: 22956823
He et al (2012) Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR. Neuropsychopharmacology 37 1338 PMID: 22218089
Lobb et al (2010) A dynamic role for GABA receptors on the firing pattern of midbrain dopaminergic neurons. J Neurophysiol 104 403 PMID: 20445035
Buchanan et al (2010) Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels. Neuron 68 948 PMID: 21145007
Haj-Dahmane (2005) The wake-promoting peptide orexin-B inhibits glutamatergic transmission to dorsal raphe nucleus serotonin neurons through retrograde endocannabinoid signaling. J Neurosci 25 896 PMID: 15673670
Kinney (2005) GAT-3 transporters regulate inhibition in the neocortex. Br J Pharmacol 94 4533 PMID: 16135550
Ying and Goldstein (2005) Propofol suppresses synaptic responsiveness of somatosensory relay neurons to excitatory input by potentiating GABA(A) receptor chloride channels. Cereb Cortex 1 2 PMID: 15813991
Safo and Regehr (2005) Endocannabinoids control the induction of cerebellar LTD. Neuron 48 647 PMID: 16301180
Einstein et al (2013) Galanin-induced decreases in nucleus accumbens/striatum excitatory postsynaptic potentials and morphine conditioned place preference require both galanin receptor 1 and galanin receptor 2. Eur J Neurosci 37 1541 PMID: 23387435
Razik et al (2013) Impairment of GABA transporter GAT-1 terminates cortical recurrent network activity via enhanced phasic inhibition. Front Neural Circuits 7 141 PMID: 24062646
Ilie et al (2012) Adenosine release during seizures attenuates GABAA receptor-mediated depolarization. J Neurosci 32 5321 PMID: 22496577
Hulme et al (2012) Calcium-dependent but action potential-independent BCM-like metaplasticity in the hippocampus. J Neurosci 32 6785 PMID: 22593048
Zhu et al (2012) Inflammation-induced shift in spinal GABA(A) signaling is associated with a tyrosine kinase-dependent increase in GABA(A) current density in nociceptive afferents. J Neurophysiol 108 2581 PMID: 22914654
Hoffman et al (2010) Control of cannabinoid CB1 receptor function on glutamate axon terminals by endogenous adenosine acting at A1 receptors. J Neurosci 30 545 PMID: 20071517
Zhang et al (2010) Cannabinoid CB1 receptor facilitation of substance P release in the rat spinal cord, measured as neurokinin 1 receptor internalization. Eur J Neurosci 31 225 PMID: 20074214
Balakrishnan et al (2009) Slow glycinergic transmission mediated by transmitter pooling. Nat Neurosci 12 286 PMID: 19198604
Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551 PMID: 15140926
Colavita et al (2016) Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus. Sci Rep 6 28454 PMID: 27345695
Pennock et al (2012) Multiple inhibitory G-protein-coupled receptors resist acute desensitization in the presynaptic but not postsynaptic compartments of neurons. J Neurosci 32 10192 PMID: 22836254
Wu et al (2011) Ovarian hormone deficiency reduces intrinsic excitability and abolishes acute estrogen sensitivity in hippocampal CA1 pyramidal neurons. J Neurosci 31 2638 PMID: 21325532
Zhang and Buckmaster (2009) Dysfunction of the dentate basket cell circuit in a rat model of temporal lobe epilepsy. Neuropharmacology 29 7846 PMID: 19535596
Dargan et al (2009) ACET is a highly potent and specific kainate receptor antagonist: characterisation and effects on hippocampal mossy fibre function. Neuropharmacology 56 121 PMID: 18789344
Hellier et al (2009) NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy. Neuropharmacology 56 414 PMID: 18930747
Owen and Grover (2015) Activity-dependent differences in function between proximal and distal Schaffer collaterals. J Neurophysiol 113 3646 PMID: 25855695
Wang et al (2014) GABAB receptors expressed in human aortic endothelial cells mediate intracellular calcium concentration regulation and endothelial nitric oxide synthase translocation. J Cereb Blood Flow Metab 2014 871735 PMID: 25114926
Hayama et al (2013) GABA promotes the competitive selection of dendritic spines by controlling local Ca2+ signaling. Nat Neurosci 16 1409 PMID: 23974706
Cruz et al (2013) Ghrelin increases GABAergic transmission and interacts with ethanol actions in the rat central nucleus of the amygdala. Neuropsychopharmacology 38 364 PMID: 22968812
Araragi et al (2013) Conservation of 5-HT1A receptor-mediated autoinhibition of serotonin (5-HT) neurons in mice with altered 5-HT homeostasis. Front Pharmacol 4 97 PMID: 23935583
Errington et al (2011) Aberrant GABA(A) receptor-mediated inhibition in cortico-thalamic networks of succinic semialdehyde dehydrogenase deficient mice. PLoS One 6 e19021 PMID: 21526163
Wood et al (2000) The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. J Neurosci 131 1050 PMID: 11082110
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Effects of GABAB activation on electrically stimulated dopamine release in the striatum was measured using fast scan cyclic votlammetry. CGP55845 (200nM) nicely reverse Baclofen (30uM) effects on dopamine release.
We typically make a 10mM stock solution in DMSO. Drug seems pretty stable.
Literature in this Area
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