Home / GABA-B Receptor Antagonists / CGP 55845 hydrochloride

CGP 55845 hydrochloride

Catalog #: 1248
105 Citations Datasheet / COA / SDS
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1248/10
1248/50
CGP 55845 hydrochloride | CAS No. 149184-22-5 | GABA-B Receptor Antagonists
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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%

Product Details
Citations (105)
Supplemental Products
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of Novartis Pharma AG

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. Neurogliaform cells dynamically regulate somatosensory integration via synapse-specific modulation.
    Chittajallu, Ramesh, Pelkey, Kenneth, McBain, Chris J
    Nat Neurosci, 2013;16(1):13-5.
  3. Cell type-specific properties of subicular GABAergic currents shape hippocampal output firing mode.
    Panuccio, Gabriell, Vicini, Stefano, Avoli, Massimo
    PLoS ONE, 2012;7(12):e50241.
  4. gamma-Aminobutyric Acid Type B (GABAB) Receptor Expression Is Needed for Inhibition of N-type (Cav2.2) Calcium Channels by Analgesic alpha-Conotoxins.
    Cuny H, de Faoite A, Huynh TG, Yasuda T, Berecki G, Adams DJ
    J. Biol. Chem., 2012;287(28):23948-57.
  5. Impaired chemosensitivity of mouse dorsal raphe serotonergic neurons overexpressing serotonin 1A (Htr1a) receptors.
    Baccini G, Mlinar B, Audero E, Gross C, Corradetti R
    PLoS ONE, 2012;7(9):e45072.
  6. Central amygdala circuits mediate hyperalgesia in alcohol-dependent rats
    EM Avegno, TD Lobell, CA Itoga, BB Baynes, AM Whitaker, MM Weera, S Edwards, JW Middleton, NW Gilpin
    J. Neurosci., 2018;0(0):.
  7. Evidence for pharmacologically distinct GABAB receptors associated with cAMP production in rat brain.
    Cunninghan and Enna
    Brain Res., 1996;720:220
  8. The GABAB antagonist CGP 55845A reduces presynaptic GABA1 actions in neurons of the rat in vitro.
    Deisz
    Neuroscience, 1999;93:1241
  9. 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
  10. Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body.
    Zhang et al.
    J.Physiol., 2007;578:735
  11. 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
  12. Potent, orally active GABAB receptor antagonists.
    Froestl et al.
    Pharmacol.Rev.Comm., 1996;8:127
  13. Brainstem activation of GABAB receptors in the nucleus tractus solitarius increases gastric motility
    L Bellusci, E Kim, S Garcia DuB, RA Gillis, S Vicini, N Sahibzada
    Frontiers in Neuroscience, 2022;16(0):961042.

Product Datasheets

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Citations for CGP 55845 hydrochloride

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

105 Citations: Showing 1 - 10

  1. Oxytocin in the anterior cingulate cortex attenuates neuropathic pain and emotional anxiety by inhibiting presynaptic long-term potentiation
    Authors: Li Et al.
    Cell Rep  2021;36:109411
  2. Axonal mechanisms mediating γ-aminobutyric acid receptor type A (GABA-A) inhibition of striatal dopamine release.
    Authors: Kramer Et al.
    ELife  2020;9:e55729
  3. Functional Dissection of Basal Ganglia Inhibitory Inputs onto Substantia Nigra Dopaminergic Neurons
    Authors: Evans Et al.
    Cell Rep  2020;32:108156
  4. Electrophysiological evaluation of extracellular spermine and alkaline pH on synaptic human GABAA receptors.
    Authors: Limó n Et al.
    Transl Psychiatry  2019;9:218
  5. Synapse-specific opioid modulation of thalamo-cortico-striatal circuits.
    Authors: Birdsong Et al.
    Elife  2019;8
  6. GABARAPs dysfunction by autophagy deficiency in adolescent brain impairs GABAA receptor trafficking and social behavior.
    Authors: Hui Et al.
    Sci Adv  2019;5:eaau8237
  7. Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference.
    Authors: Nam Et al.
    Cell Rep  2019;28:1154
  8. Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons.
    Authors: Livingstone Et al.
    Front Mol Neurosci  2019;12:198
  9. A hippocampal circuit linking dorsal CA2 to ventral CA1 critical for social memory dynamics.
    Authors: Meira Et al.
    Nat.Commun.  2018;9:4163
  10. Salicylate-Induced Suppression of Electrically Driven Activity in Brain Slices from the Auditory Cortex of Aging Mice.
    Authors: Namikawa Et al.
    Front Aging Neurosci  2018;9:395
  11. Potassium channels contribute to activity-dependent regulation of dendritic inhibition.
    Authors: Chang and Higley
    Physiol Rep  2018;6:e13747
  12. A circuit from hippocampal CA2 to lateral septum disinhibits social aggression.
    Authors: Leroy Et al.
    Nature  2018;564:213
  13. JIP1-Mediated JNK Activation Negatively Regulates Synaptic Plasticity and Spatial Memory.
    Authors: Morel Et al.
    J Neurosci  2018;38:3708
  14. DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate.
    Authors: Cai and Ford
    Cell Rep  2018;25:3148
  15. Local GABAA receptor mediated suppression of DA release within the nucleus accumbens.
    Authors: Brodnik Et al.
    ACS Chem Neurosci  2018;17:1978
  16. LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance.
    Authors: Hashimotodani Et al.
    Neuron  2017;95:928
  17. Proximodistal Heterogeneity of Hippocampal CA3 Pyramidal Neuron Intrinsic Properties, Connectivity, and Reactivation during Memory Recall.
    Authors: Sun Et al.
    Neuron  2017;95:656
  18. Input-Timing-Dependent Plasticity in the Hippocampal CA2 Region and Its Potential Role in Social Memory.
    Authors: Leroy Et al.
    Neuron  2017;95:1089
  19. Chronic Loss of CA2 Transmission Leads to Hippocampal Hyperexcitability.
    Authors: Boehringer Et al.
    Neuron  2017;94:642
  20. Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells.
    Authors: Hirono
    Neuropharmacology  2017;118:79
  21. Differential Somatic Ca2+ Channel Profile in Midbrain DArgic Neurons
    Authors: Philippart Et al.
    The Journal of Neuroscience  2016;6:7234
  22. Nicotinic and opioid receptor regulation of striatal DA D2-receptor mediated transmission
    Authors: Mamaligas Et al.
    Scientific Reports  2016;6:37834
  23. The chemokine CXCL16 modulates neurotransmitter release in hippocampal CA1 area
    Authors: Di Castro Et al.
    Scientific Reports  2016;6:34633
  24. Increased GABAB receptor signaling in a rat model for schizophrenia
    Authors: Selten Et al.
    Scientific Reports  2016;6:34240
  25. Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.
    Authors: Colavita Et al.
    Sci Rep  2016;6:28454
  26. 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
  27. Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus.
    Authors: Dennis Et al.
    J Neurophysiol  2016;26:414
  28. 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
  29. Vasculo-neuronal coupling: retrograde vascular communication to brain neurons
    Authors: Jung Kim Et al.
    The Journal of Neuroscience  2016;14:12624
  30. 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
  31. 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
  32. Distinct regulation of DA D2S and D2L autoreceptor signaling by calcium.
    Authors: Gantz Et al.
    PLoS One  2015;4
  33. Prototypic and arkypallidal neurons in the DA-intact external globus pallidus.
    Authors: Abdi Et al.
    Elife  2015;35:6667
  34. Absence of plateau potentials in dLGN cells leads to a breakdown in retinogeniculate refinement.
    Authors: Dilger Et al.
    J Neurosci  2015;35:3652
  35. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci  2015;35:11252
  36. Neurotensin Induces Presynaptic Depression of D2 DA Autoreceptor-Mediated Neurotransmission in Midbrain DArgic Neurons.
    Authors: Piccart Et al.
    J Neurosci  2015;35:11144
  37. 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
  38. Activity-dependent differences in function between proximal and distal Schaffer collaterals.
    Authors: Owen and Grover
    J Neurophysiol  2015;113:3646
  39. Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice.
    Authors: Wang Et al.
    J Neurophysiol  2015;10:e0139332
  40. 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
  41. 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
  42. Phasic DA release drives rapid activation of striatal D2-receptors.
    Authors: Marcott Et al.
    Neuron  2014;84:164
  43. Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex.
    Authors: Muralidhar Et al.
    Front Neuroanat  2014;7:52
  44. 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
  45. 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
  46. 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
  47. 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
  48. Dentate gyrus network dysfunctions precede the symptomatic phase in a genetic mouse model of seizures.
    Authors: Toader Et al.
    Nat Commun  2013;7:138
  49. 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
  50. 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
  51. 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
  52. Galanin-induced decreases in nucleus accumbens/striatum excitatory postsynaptic potentials and mor. conditioned place preference require both galanin receptor 1 and galanin receptor 2.
    Authors: Einstein Et al.
    Eur J Neurosci  2013;37:1541
  53. Ovarian hormone loss impairs excitatory synaptic transmission at hippocampal CA3-CA1 synapses.
    Authors: Wu Et al.
    J Neurosci  2013;33:16158
  54. TRPM2 channels are required for NMDA-induced burst firing and contribute to H(2)O(2)-dependent modulation in substantia nigra pars reticulata GABAergic neurons.
    Authors: Lee Et al.
    J Neurosci  2013;33:1157
  55. GABA promotes the competitive selection of dendritic spines by controlling local Ca2+ signaling.
    Authors: Hayama Et al.
    Nat Neurosci  2013;16:1409
  56. 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
  57. 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
  58. Calcium-dependent but action potential-independent BCM-like metaplasticity in the hippocampus.
    Authors: Hulme Et al.
    J Neurosci  2012;32:6785
  59. Adenosine release during seizures attenuates GABAA receptor-mediated depolarization.
    Authors: Ilie Et al.
    J Neurosci  2012;32:5321
  60. 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
  61. Multiple inhibitory G-protein-coupled receptors resist acute desensitization in the presynaptic but not postsynaptic compartments of neurons.
    Authors: Pennock Et al.
    J Neurosci  2012;32:10192
  62. Persistent inflammation increases GABA-induced depolarization of rat cutaneous dorsal root ganglion neurons in vitro.
    Authors: Zhu Et al.
    Neurobiol Dis  2012;220:330
  63. Astrocytes mediate in vivo cholinergic-induced synaptic plasticity.
    Authors: Navarrete Et al.
    PLoS Biol  2012;10:e1001259
  64. 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
  65. 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
  66. Diffuse and specific tectopulvinar terminals in the tree shrew: synapses, synapsins, and synaptic potentials.
    Authors: Wei Et al.
    PLoS One  2011;6:e23781
  67. 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
  68. Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1.
    Authors: Zschenderlein Et al.
    PLoS One  2011;6:e16116
  69. 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
  70. Ovarian hormone deficiency reduces intrinsic excitability and abolishes acute estrogen sensitivity in hippocampal CA1 pyramidal neurons.
    Authors: Wu Et al.
    J Neurosci  2011;31:2638
  71. SK2 channels are neuroprotective for ischemia-induced neuronal cell death.
    Authors: Allen Et al.
    Neuroscience  2011;31:2302
  72. 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
  73. Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1.
    Authors: Straub Et al.
    Nat Neurosci  2011;14:866
  74. The SK2-long isoform directs synaptic localization and function of SK2-containing channels.
    Authors: Allen Et al.
    Nat Neurosci  2011;14:744
  75. Suppression of PKR promotes network excitability and enhanced cognition by IF.-γ-mediated disinhibition.
    Authors: Zhu Et al.
    Cell  2011;147:1384
  76. 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
  77. Cannabinoid CB1 receptor facilitation of substance P release in the rat spinal cord, measured as neurokinin 1 receptor internalization.
    Authors: Zhang Et al.
    Eur J Neurosci  2010;31:225
  78. 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
  79. Control of cannabinoid CB1 receptor function on glutamate axon terminals by endogenous adenosine acting at A1 receptors.
    Authors: Hoffman Et al.
    J Neurosci  2010;30:545
  80. A dynamic role for GABA receptors on the firing pattern of midbrain DArgic neurons.
    Authors: Lobb Et al.
    J Neurophysiol  2010;104:403
  81. NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy.
    Authors: Hellier Et al.
    Neuropharmacology  2009;56:414
  82. 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
  83. Dysfunction of the dentate basket cell circuit in a rat model of temporal lobe epilepsy.
    Authors: Zhang and Buckmaster
    Neuropharmacology  2009;29:7846
  84. Slow glycinergic transmission mediated by transmitter pooling.
    Authors: Balakrishnan Et al.
    Nat Neurosci  2009;12:286
  85. Co-transmission of DA and GABA in periglomerular cells.
    Authors: Maher and Westbrook
    J Neurosci  2008;99:1559
  86. Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys.
    Authors: Darbin and Wichmann
    J Neurophysiol  2008;99:1294
  87. 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
  88. Autonomous initiation and propagation of action potentials in neurons of the subthalamic nucleus.
    Authors: Atherton Et al.
    J Physiol  2008;586:5679
  89. Input-specific plasticity at excitatory synapses mediated by endocannabinoids in the dentate gyrus.
    Authors: Chiu and Castillo
    Neuropharmacology  2008;54:68
  90. Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others.
    Authors: Karson Et al.
    Biomed Res Int  2008;54:117
  91. Alpha1-adrenergic receptor-induced heterosynaptic long-term depression in the bed nucleus of the stria terminalis is disrupted in mouse models of affective disorders.
    Authors: McElligott
    Neuropsychopharmacology  2008;33:2313
  92. Dichotomous DArgic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science  2008;321:848
  93. 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
  94. Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons.
    Authors: Molineux Et al.
    J Neurosci  2008;100:2684
  95. 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
  96. Brain injury impairs dentate gyrus inhibitory efficacy.
    Authors: Bonislawski Et al.
    J Neurophysiol  2007;25:163
  97. 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
  98. 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
  99. GAT-3 transporters regulate inhibition in the neocortex.
    Authors: Kinney
    Br J Pharmacol  2005;94:4533
  100. A parametric assessment of GABA antagonist effects on paired-pulse facilitation in the rat anterior cingulate cortex.
    Authors: Sylantyev Et al.
    Neurosci Res  2005;52:362
  101. Endocannabinoids control the induction of cerebellar LTD.
    Authors: Safo and Regehr
    Neuron  2005;48:647
  102. The wake-promoting peptide orexin-B inhibits glutamatergic transmission to dorsal raphe nucleus serotonin neurons through retrograde endocannabinoid signaling.
    Authors: Haj-Dahmane
    J Neurosci  2005;25:896
  103. PropF. 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
  104. Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
    Authors: Huang Et al.
    J Neurosci  2004;24:4551
  105. 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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