CGP 55845 hydrochloride

Cat. No. 1248

CGP 55845 hydrochloride C18H22Cl2NO3P.HCl [149184-22-5]

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Chemical Name: (2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride

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

Technical Data

M.Wt:
438.71
Formula:
C18H22Cl2NO3P.HCl
Solubility:
Soluble to 100 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at RT
CAS No:
149184-22-5

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
Select another batch:

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.

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.

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Cunninghan and Enna (1996) Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain. Brain Res. 720 220. PMID: 8782915.

Froestl et al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8 127.

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.

If you know of a relevant reference for this product please let us know.

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

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.

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.

Abdi et al (2015) Prototypic and arkypallidal neurons in the dopamine-intact external globus pallidus. Elife 35 6667. PMID: 25926446.

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.

Dilger et al (2015) Absence of plateau potentials in dLGN cells leads to a breakdown in retinogeniculate refinement. J Neurosci 35 3652. PMID: 25716863.

Gantz et al (2015) Distinct regulation of dopamine D2S and D2L autoreceptor signaling by calcium. PLoS One 4. PMID: 26308580.

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.

Tabatadze et al (2015) Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus. J Neurosci 35 11252. PMID: 26269634.

Wang et al (2015) Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice. J Neurophysiol 10 e0139332. PMID: 26418566.

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.

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.

Muralidhar et al (2014) Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex. Front Neuroanat 7 52. PMID: 24474905.

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.

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.

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.

Hayama et al (2013) GABA promotes the competitive selection of dendritic spines by controlling local Ca2+ signaling. Nat Neurosci 16 1409. PMID: 23974706.

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.

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.

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.

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.

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.

Navarrete et al (2012) Astrocytes mediate in vivo cholinergic-induced synaptic plasticity. PLoS Biol 10 e1001259. PMID: 22347811.

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.

Allen et al (2011) The SK2-long isoform directs synaptic localization and function of SK2-containing channels. Nat Neurosci 14 744. PMID: 21602822.

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.

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.

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.

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.

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.

Lobb et al (2010) A dynamic role for GABA receptors on the firing pattern of midbrain dopaminergic neurons. J Neurophysiol 104 403. PMID: 20445035.

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.

Atherton et al (2008) Autonomous initiation and propagation of action potentials in neurons of the subthalamic nucleus. J Physiol 586 5679. PMID: 18832425.

Darbin and Wichmann (2008) Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys. J Neurophysiol 99 1294. PMID: 18216224.

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.

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.

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

Shen et al (2008) Dichotomous dopaminergic control of striatal synaptic plasticity. Science 321 848. PMID: 18687967.

Bonislawski et al (2007) Brain injury impairs dentate gyrus inhibitory efficacy. J Neurophysiol 25 163. PMID: 17045484.

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.

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.

Kinney (2005) GAT-3 transporters regulate inhibition in the neocortex. Br J Pharmacol 94 4533. PMID: 16135550.

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

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.

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.

Do you know of a great paper that uses CGP 55845 hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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