CGP 55845 hydrochloride

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Cat.No. 1248 - CGP 55845 hydrochloride | C18H22Cl2NO3P.HCl | CAS No. 149184-22-5
Description: Potent, selective GABAB antagonist
Chemical Name: (2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (63)
Reviews
Literature

Biological Activity

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

CGP 55845 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.87 100mM 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Keywords: CGP 55845 hydrochloride, supplier, Potent, selective, GABAB, antagonists, Receptors, CGP55845, hydrochloride, GABAB, Receptors, GABAB, Receptors, Tocris Bioscience

63 Citations for CGP 55845 hydrochloride

Citations are publications that use Tocris products. Selected citations for CGP 55845 hydrochloride include:

Hirono (2017) Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells. Neuropharmacology 118 79 PMID: 28300552

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

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

Dennis et al (2016) Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus. J Neurophysiol 26 414 PMID: 26472558

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

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

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

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

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

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

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 (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

Allen et al (2011) SK2 channels are neuroprotective for ischemia-induced neuronal cell death. Neuroscience 31 2302 PMID: 21712833

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

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

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

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

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

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

Zhang and Buckmaster (2009) Dysfunction of the dentate basket cell circuit in a rat model of temporal lobe epilepsy. Neuropharmacology 29 7846 PMID: 19535596

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

Molineux et al (2008) Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons. J Neurosci 100 2684 PMID: 18768644

Karson et al (2008) Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others. Biomed Res Int 54 117 PMID: 17689570

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

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

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

Safo and Regehr (2005) Endocannabinoids control the induction of cerebellar LTD. Neuron 48 647 PMID: 16301180

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

Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551 PMID: 15140926


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