Catalog Number: 1248
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.
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.
Additional Information
Licensing Caveats:
Sold with the permission of Novartis Pharma AG
Background References
  1. Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain.
    Cunninghan and Enna
    Brain Res., 1996;720:220
  2. The GABAB antagonist CGP 55845A reduces presynaptic GABA1 actions in neurons of the rat in vitro.
    Deisz
    Neuroscience, 1999;93:1241
  3. 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
    Neuropharmacology, 2008;55:47
  4. GABA and glutamate release affected by GABAB receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors.
    Waldmeier et al.
    Br.J.Pharmacol., 1994;113:1515
  5. Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body.
    Zhang et al.
    J.Physiol., 2007;578:735
  6. Potent, orally active GABAB receptor antagonists.
    Froestl et al.
    Pharmacol.Rev.Comm., 1996;8:127
Citations:

The citations listed below are publications that use Tocris products. Selected citations for CGP 55845 hydrochloride include:

63 Citations: Showing 1 - 10
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  1. Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells.
    Authors: Hirono
    Neuropharmacology 2017;118:79
  2. Differential Somatic Ca2+ Channel Profile in Midbrain Dopaminergic Neurons
    Authors: Philippart Et al.
    The Journal of Neuroscience 2016;6:7234
  3. Nicotinic and opioid receptor regulation of striatal dopamine D2-receptor mediated transmission
    Authors: Mamaligas Et al.
    Scientific Reports 2016;6:37834
  4. The chemokine CXCL16 modulates neurotransmitter release in hippocampal CA1 area
    Authors: Di Castro Et al.
    Scientific Reports 2016;6:34633
  5. Increased GABAB receptor signaling in a rat model for schizophrenia
    Authors: Selten Et al.
    Scientific Reports 2016;6:34240
  6. Presynaptic GABAB receptors reduce transmission at parabrachial synapses in the lateral central amygdala by inhibiting N-type calcium channels.
    Authors: Delaney and Crane
    Sci Rep 2016;6:19255
  7. Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus.
    Authors: Dennis Et al.
    J Neurophysiol 2016;26:414
  8. Involvement of GABAB Receptor Signaling in Antipsychotic-like Action of the Novel Orthosteric Agonist of the mGlu4 Receptor, LSP4-2022
    Authors: Wozniak Et al.
    Current Neuropharmacology 2016;14:413
  9. Vasculo-neuronal coupling: retrograde vascular communication to brain neurons
    Authors: Jung Kim Et al.
    The Journal of Neuroscience 2016;14:12624
  10. Non-additive modulation of synaptic transmission by serotonin, adenosine, and cholinergic modulators in the sensory thalamus.
    Authors: Yang Et al.
    Front Cell Neurosci 2015;9:60
  11. IL-1 interacts with ethanol effects on GABAergic transmission in the mouse central amygdala.
    Authors: Bajo Et al.
    Am J Physiol Gastrointest Liver Physiol 2015;6:49
  12. Distinct regulation of dopamine D2S and D2L autoreceptor signaling by calcium.
    Authors: Gantz Et al.
    PLoS One 2015;4
  13. Prototypic and arkypallidal neurons in the dopamine-intact external globus pallidus.
    Authors: Abdi Et al.
    Elife 2015;35:6667
  14. Absence of plateau potentials in dLGN cells leads to a breakdown in retinogeniculate refinement.
    Authors: Dilger Et al.
    J Neurosci 2015;35:3652
  15. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci 2015;35:11252
  16. Neurotensin Induces Presynaptic Depression of D2 Dopamine Autoreceptor-Mediated Neurotransmission in Midbrain Dopaminergic Neurons.
    Authors: Piccart Et al.
    J Neurosci 2015;35:11144
  17. Asynchronous GABA Release Is a Key Determinant of Tonic Inhibition and Controls Neuronal Excitability: A Study in the Synapsin II-/- Mouse.
    Authors: Medrihan Et al.
    Cereb Cortex 2015;25:3356
  18. Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice.
    Authors: Wang Et al.
    J Neurophysiol 2015;10:e0139332
  19. Inhibitory glycinergic neurotransmission in the mammalian auditory brainstem upon prolonged stimulation: short-term plasticity and synaptic reliability.
    Authors: Kramer Et al.
    Front Neural Circuits 2014;8:14
  20. Phasic dopamine release drives rapid activation of striatal D2-receptors.
    Authors: Marcott Et al.
    Neuron 2014;84:164
  21. Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex.
    Authors: Muralidhar Et al.
    Front Neuroanat 2014;7:52
  22. 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.
    Authors: Qi Et al.
    Acta Neuropathol Commun 2014;2:175
  23. GABAB receptors expressed in human aortic endothelial cells mediate intracellular calcium concentration regulation and endothelial nitric oxide synthase translocation.
    Authors: Wang Et al.
    J Cereb Blood Flow Metab 2014;2014:871735
  24. Dentate gyrus network dysfunctions precede the symptomatic phase in a genetic mouse model of seizures.
    Authors: Toader Et al.
    Nat Commun 2013;7:138
  25. Conservation of 5-HT1A receptor-mediated autoinhibition of serotonin (5-HT) neurons in mice with altered 5-HT homeostasis.
    Authors: Araragi Et al.
    Front Pharmacol 2013;4:97
  26. Synapsin II desynchronizes neurotransmitter release at inhibitory synapses by interacting with presynaptic calcium channels.
    Authors: Medrihan Et al.
    Proc Natl Acad Sci U S A 2013;4:1512
  27. Ghrelin increases GABAergic transmission and interacts with ethanol actions in the rat central nucleus of the amygdala.
    Authors: Cruz Et al.
    Neuropsychopharmacology 2013;38:364
  28. GABA promotes the competitive selection of dendritic spines by controlling local Ca2+ signaling.
    Authors: Hayama Et al.
    Nat Neurosci 2013;16:1409
  29. Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus.
    Authors: Jurgens Et al.
    PLoS One 2012;7:e45717
  30. Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR.
    Authors: He Et al.
    Neuropsychopharmacology 2012;37:1338
  31. Repeated stress dysregulates κ-opioid receptor signaling in the dorsal raphe through a p38α MAPK-dependent mechanism.
    Authors: Lemos Et al.
    J Neurosci 2012;32:12325
  32. Persistent inflammation increases GABA-induced depolarization of rat cutaneous dorsal root ganglion neurons in vitro.
    Authors: Zhu Et al.
    Neurobiol Dis 2012;220:330
  33. Astrocytes mediate in vivo cholinergic-induced synaptic plasticity.
    Authors: Navarrete Et al.
    PLoS Biol 2012;10:e1001259
  34. Intermediate conductance calcium-activated potassium channels modulate summation of parallel fiber input in cerebellar Purkinje cells.
    Authors: Engbers Et al.
    J Neurosci 2012;109:2601
  35. Diffuse and specific tectopulvinar terminals in the tree shrew: synapses, synapsins, and synaptic potentials.
    Authors: Wei Et al.
    PLoS One 2011;6:e23781
  36. Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1.
    Authors: Zschenderlein Et al.
    PLoS One 2011;6:e16116
  37. Requirements for synaptically evoked plateau potentials in relay cells of the dorsal lateral geniculate nucleus of the mouse.
    Authors: Dilger Et al.
    J Physiol 2011;589:919
  38. SK2 channels are neuroprotective for ischemia-induced neuronal cell death.
    Authors: Allen Et al.
    Neuroscience 2011;31:2302
  39. Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry.
    Authors: Hays Et al.
    J Neurosci 2011;31:14223
  40. Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1.
    Authors: Straub Et al.
    Nat Neurosci 2011;14:866
  41. The SK2-long isoform directs synaptic localization and function of SK2-containing channels.
    Authors: Allen Et al.
    Nat Neurosci 2011;14:744
  42. Suppression of PKR promotes network excitability and enhanced cognition by interferon-γ-mediated disinhibition.
    Authors: Zhu Et al.
    Cell 2011;147:1384
  43. Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels.
    Authors: Buchanan Et al.
    Neuron 2010;68:948
  44. M3 muscarinic acetylcholine receptor expression confers differential cholinergic modulation to neurochemically distinct hippocampal basket cell subtypes.
    Authors: Rio Et al.
    Front Pharmacol 2010;30:6011
  45. A dynamic role for GABA receptors on the firing pattern of midbrain dopaminergic neurons.
    Authors: Lobb Et al.
    J Neurophysiol 2010;104:403
  46. NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy.
    Authors: Hellier Et al.
    Neuropharmacology 2009;56:414
  47. ACET is a highly potent and specific kainate receptor antagonist: characterisation and effects on hippocampal mossy fibre function.
    Authors: Dargan Et al.
    Neuropharmacology 2009;56:121
  48. Dysfunction of the dentate basket cell circuit in a rat model of temporal lobe epilepsy.
    Authors: Zhang and Buckmaster
    Neuropharmacology 2009;29:7846
  49. Co-transmission of dopamine and GABA in periglomerular cells.
    Authors: Maher and Westbrook
    J Neurosci 2008;99:1559
  50. Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys.
    Authors: Darbin and Wichmann
    J Neurophysiol 2008;99:1294
  51. Neuropeptide S-mediated control of fear expression and extinction: role of intercalated GABAergic neurons in the amygdala.
    Authors: Jüngling Et al.
    Neuron 2008;59:298
  52. Autonomous initiation and propagation of action potentials in neurons of the subthalamic nucleus.
    Authors: Atherton Et al.
    J Physiol 2008;586:5679
  53. Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others.
    Authors: Karson Et al.
    Biomed Res Int 2008;54:117
  54. Dichotomous dopaminergic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science 2008;321:848
  55. Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons.
    Authors: Molineux Et al.
    J Neurosci 2008;100:2684
  56. Brain injury impairs dentate gyrus inhibitory efficacy.
    Authors: Bonislawski Et al.
    J Neurophysiol 2007;25:163
  57. Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices.
    Authors: Fukunaga Et al.
    Br J Pharmacol 2007;151:870
  58. Glial glutamate transporters maintain one-to-one relationship at the climbing fiber-Purkinje cell synapse by preventing glutamate spillover.
    Authors: Takayasu Et al.
    Mol Pain 2006;26:6563
  59. GAT-3 transporters regulate inhibition in the neocortex.
    Authors: Kinney
    Br J Pharmacol 2005;94:4533
  60. Endocannabinoids control the induction of cerebellar LTD.
    Authors: Safo and Regehr
    Neuron 2005;48:647
  61. Propofol suppresses synaptic responsiveness of somatosensory relay neurons to excitatory input by potentiating GABA(A) receptor chloride channels.
    Authors: Ying and Goldstein
    Cereb Cortex 2005;1:2
  62. Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
    Authors: Huang Et al.
    J Neurosci 2004;24:4551
  63. The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
    Authors: Wood Et al.
    J Neurosci 2000;131:1050
Expand to show all 63 Citations

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