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Submit ReviewCGP 55845 hydrochloride
Description: Potent and selective GABAB antagonist
Chemical Name: (2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for CGP 55845 hydrochloride
CGP 55845 hydrochloride is a 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.
Licensing Information
Sold with the permission of Novartis Pharma AG
Compound Libraries for CGP 55845 hydrochloride
CGP 55845 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CGP 55845 hydrochloride
| M. Wt | 438.71 |
| Formula | C18H22Cl2NO3P.HCl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 149184-22-5 |
| PubChem ID | 5311042 |
| InChI Key | ZODSPDOOCZZEIM-BBRMVZONSA-N |
| Smiles | Cl.C[C@H](NC[C@H](O)CP(O)(=O)CC1=CC=CC=C1)C1=CC=C(Cl)C(Cl)=C1 |
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.
Solubility Data for CGP 55845 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.87 | 100 with gentle warming |
Preparing Stock Solutions for CGP 55845 hydrochloride
The following data is based on the product molecular weight 438.71. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for CGP 55845 hydrochloride
References for CGP 55845 hydrochloride
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
105 Citations for CGP 55845 hydrochloride
Citations are publications that use Tocris products. Selected citations for CGP 55845 hydrochloride include:
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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
Namikawa et al (2018) Salicylate-Induced Suppression of Electrically Driven Activity in Brain Slices from the Auditory Cortex of Aging Mice. Front Aging Neurosci 9 395 PMID: 29311894
Morel et al (2018) JIP1-Mediated JNK Activation Negatively Regulates Synaptic Plasticity and Spatial Memory. J Neurosci 38 3708 PMID: 29540552
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Cai and Ford (2018) DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate. Cell Rep 25 3148 PMID: 30540946
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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
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
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Zhu et al (2011) Suppression of PKR promotes network excitability and enhanced cognition by IF.-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
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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
Philippart et al (2016) Differential Somatic Ca2+ Channel Profile in Midbrain DArgic 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
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
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Kramer et al (2020) Axonal mechanisms mediating γ-aminobutyric acid receptor type A (GABA-A) inhibition of striatal dopamine release. ELife 9 e55729 PMID: 32870779
Evans et al (2020) Functional Dissection of Basal Ganglia Inhibitory Inputs onto Substantia Nigra Dopaminergic Neurons Cell Rep 32 108156 PMID: 32937133
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
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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
Li et al (2021) Oxytocin in the anterior cingulate cortex attenuates neuropathic pain and emotional anxiety by inhibiting presynaptic long-term potentiation Cell Rep 36 109411 PMID: 34289348
Hashimotodani et al (2017) LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance. Neuron 95 928 PMID: 28817805
Boehringer et al (2017) Chronic Loss of CA2 Transmission Leads to Hippocampal Hyperexcitability. Neuron 94 642 PMID: 28472661
Sun et al (2017) Proximodistal Heterogeneity of Hippocampal CA3 Pyramidal Neuron Intrinsic Properties, Connectivity, and Reactivation during Memory Recall. Neuron 95 656 PMID: 28772124
Leroy et al (2017) Input-Timing-Dependent Plasticity in the Hippocampal CA2 Region and Its Potential Role in Social Memory. Neuron 95 1089 PMID: 28823730
Einstein et al (2013) Galanin-induced decreases in nucleus accumbens/striatum excitatory postsynaptic potentials and mor. 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
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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
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Limó n et al (2019) Electrophysiological evaluation of extracellular spermine and alkaline pH on synaptic human GABAA receptors. Transl Psychiatry 9 218 PMID: 31488811
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Reviews for CGP 55845 hydrochloride
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CGP-55845 increases field potential amplitudes in cortex tissue.
By
Anonymous on 06/07/2019
Assay Type: Ex Vivo
Species: Rat
Cell Line/Tissue: Anterior cingulate cortex
CGP-55845 was used to study input of GABA-B receptors into field potential generation in anterior cingulate cortex. Application of 10 nM CGP-55845 increased significantly amplitudes of field potentials and reduced their paired-pulse ratio.
Should be sonicated when dissolved.
CGP55845 reverses Baclofen effects on dopamine release..
By
Anonymous on 03/28/2018
Assay Type: Ex Vivo
Species: Mouse
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.
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