CGP 55845 hydrochloride

  ( 75 citations ) ( 1 Review )    
Product Datasheet
Catalog Number:1248
Chemical Name:(2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride
Product Details
Citations (75)
Supplemental Products
Reviews
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
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Citations:

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

75 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. Activity-dependent differences in function between proximal and distal Schaffer collaterals.
    Authors: Owen and Grover
    J Neurophysiol  2015;113:3646
  19. Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice.
    Authors: Wang Et al.
    J Neurophysiol  2015;10:e0139332
  20. Embryonic GABA(B) receptor blockade alters cell migration, adult hypothalamic structure, and anxiety- and depression-like behaviors sex specifically in mice.
    Authors: Stratton Et al.
    PLoS One  2014;9:e106015
  21. 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
  22. Phasic dopamine release drives rapid activation of striatal D2-receptors.
    Authors: Marcott Et al.
    Neuron  2014;84:164
  23. Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex.
    Authors: Muralidhar Et al.
    Front Neuroanat  2014;7:52
  24. Nociceptin/orphanin FQ decreases glutamate transmission and blocks ethanol-induced effects in the central amygdala of naive and ethanol-dependent rats.
    Authors: Kallupi Et al.
    Neuropsychopharmacology  2014;39:1081
  25. 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
  26. 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
  27. Impairment of GABA transporter GAT-1 terminates cortical recurrent network activity via enhanced phasic inhibition.
    Authors: Razik Et al.
    Front Neural Circuits  2013;7:141
  28. Dentate gyrus network dysfunctions precede the symptomatic phase in a genetic mouse model of seizures.
    Authors: Toader Et al.
    Nat Commun  2013;7:138
  29. 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
  30. 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
  31. 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
  32. Galanin-induced decreases in nucleus accumbens/striatum excitatory postsynaptic potentials and morphine conditioned place preference require both galanin receptor 1 and galanin receptor 2.
    Authors: Einstein Et al.
    Eur J Neurosci  2013;37:1541
  33. GABA promotes the competitive selection of dendritic spines by controlling local Ca2+ signaling.
    Authors: Hayama Et al.
    Nat Neurosci  2013;16:1409
  34. 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
  35. 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
  36. Calcium-dependent but action potential-independent BCM-like metaplasticity in the hippocampus.
    Authors: Hulme Et al.
    J Neurosci  2012;32:6785
  37. Adenosine release during seizures attenuates GABAA receptor-mediated depolarization.
    Authors: Ilie Et al.
    J Neurosci  2012;32:5321
  38. 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
  39. Persistent inflammation increases GABA-induced depolarization of rat cutaneous dorsal root ganglion neurons in vitro.
    Authors: Zhu Et al.
    Neurobiol Dis  2012;220:330
  40. Astrocytes mediate in vivo cholinergic-induced synaptic plasticity.
    Authors: Navarrete Et al.
    PLoS Biol  2012;10:e1001259
  41. 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
  42. Inflammation-induced shift in spinal GABA(A) signaling is associated with a tyrosine kinase-dependent increase in GABA(A) current density in nociceptive afferents.
    Authors: Zhu Et al.
    J Neurophysiol  2012;108:2581
  43. Diffuse and specific tectopulvinar terminals in the tree shrew: synapses, synapsins, and synaptic potentials.
    Authors: Wei Et al.
    PLoS One  2011;6:e23781
  44. Aberrant GABA(A) receptor-mediated inhibition in cortico-thalamic networks of succinic semialdehyde dehydrogenase deficient mice.
    Authors: Errington Et al.
    PLoS One  2011;6:e19021
  45. Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1.
    Authors: Zschenderlein Et al.
    PLoS One  2011;6:e16116
  46. 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
  47. SK2 channels are neuroprotective for ischemia-induced neuronal cell death.
    Authors: Allen Et al.
    Neuroscience  2011;31:2302
  48. 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
  49. Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1.
    Authors: Straub Et al.
    Nat Neurosci  2011;14:866
  50. The SK2-long isoform directs synaptic localization and function of SK2-containing channels.
    Authors: Allen Et al.
    Nat Neurosci  2011;14:744
  51. Suppression of PKR promotes network excitability and enhanced cognition by interferon-γ-mediated disinhibition.
    Authors: Zhu Et al.
    Cell  2011;147:1384
  52. 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
  53. 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
  54. A dynamic role for GABA receptors on the firing pattern of midbrain dopaminergic neurons.
    Authors: Lobb Et al.
    J Neurophysiol  2010;104:403
  55. NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy.
    Authors: Hellier Et al.
    Neuropharmacology  2009;56:414
  56. 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
  57. Dysfunction of the dentate basket cell circuit in a rat model of temporal lobe epilepsy.
    Authors: Zhang and Buckmaster
    Neuropharmacology  2009;29:7846
  58. Co-transmission of dopamine and GABA in periglomerular cells.
    Authors: Maher and Westbrook
    J Neurosci  2008;99:1559
  59. Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys.
    Authors: Darbin and Wichmann
    J Neurophysiol  2008;99:1294
  60. 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
  61. Autonomous initiation and propagation of action potentials in neurons of the subthalamic nucleus.
    Authors: Atherton Et al.
    J Physiol  2008;586:5679
  62. Input-specific plasticity at excitatory synapses mediated by endocannabinoids in the dentate gyrus.
    Authors: Chiu and Castillo
    Neuropharmacology  2008;54:68
  63. Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others.
    Authors: Karson Et al.
    Biomed Res Int  2008;54:117
  64. Dichotomous dopaminergic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science  2008;321:848
  65. Competition between calcium-activated K+ channels determines cholinergic action on firing properties of basolateral amygdala projection neurons.
    Authors: Power and Sah
    J Neurosci  2008;28:3209
  66. Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons.
    Authors: Molineux Et al.
    J Neurosci  2008;100:2684
  67. Coupling of L-type Ca2+ channels to KV7/KCNQ channels creates a novel, activity-dependent, homeostatic intrinsic plasticity.
    Authors: Wu Et al.
    J Neurophysiol  2008;100:1897
  68. Brain injury impairs dentate gyrus inhibitory efficacy.
    Authors: Bonislawski Et al.
    J Neurophysiol  2007;25:163
  69. 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
  70. 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
  71. GAT-3 transporters regulate inhibition in the neocortex.
    Authors: Kinney
    Br J Pharmacol  2005;94:4533
  72. Endocannabinoids control the induction of cerebellar LTD.
    Authors: Safo and Regehr
    Neuron  2005;48:647
  73. 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
  74. Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
    Authors: Huang Et al.
    J Neurosci  2004;24:4551
  75. 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
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Other Experimental Details

Other Experimental Details We typically make a 10mM stock solution in DMSO. Drug seems pretty stable.

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