AM 251

Catalog # Availability Size / Price Qty
1117/10
1117/50
1117/1
AM 251 | CAS No. 183232-66-8 | Cannabinoid R1/CB1 Antagonists
1 Image
Description: Potent CB1 antagonist; also GPR55 agonist

Chemical Name: N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide

Purity: ≥99%

Product Details
Citations (199)
Supplemental Products
Reviews (1)

Biological Activity

Potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors. Also potent GPR55 agonist (EC50 = 39 nM) and μ-opioid receptor antagonist (Ki = 251 nM).

Fluorescent Form also available.

Technical Data

M.Wt:
555.24
Formula:
C22H21Cl2IN4O
Solubility:
Soluble to 25 mM in ethanol and to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
183232-66-8

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

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Citations for AM 251

The citations listed below are publications that use Tocris products. Selected citations for AM 251 include:

199 Citations: Showing 1 - 10

  1. Feeding induced by cannabinoids is mediated independently of the melanocortin system.
    Authors: Sinnayah Et al.
    Proc Natl Acad Sci U S A  ;3:e2202
  2. The orexigenic effect of ghrelin is mediated through central activation of the endogenous cannabinoid system.
    Authors: Kola Et al.
    Br J Pharmacol  ;3:e1797
  3. Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex.
    Authors: Lafourcade Et al.
    PLoS One  ;2:e709
  4. Expression and function of cannabinoid receptors CB1 and CB2 and their cognate cannabinoid ligands in murine embryonic stem cells.
    Authors: Jiang Et al.
    PLoS One  ;2:e641
  5. Dual mechanism of TRKB activation by anandamide through CB1 and TRPV1 receptors.
    Authors: Diniz Et al.
    PeerJ  2019;7:e6493
  6. Routing Hippocampal Information Flow through Parvalbumin Interneuron Plasticity in Area CA2.
    Authors: Nasrallah Et al.
    Cell Rep  2019;27:86
  7. Endocannabinoid Signaling Mediates Local Dendritic Coordination between Excitatory and Inhibitory Synapses.
    Authors: Hu Et al.
    Cell Rep  2019;27:666
  8. Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells.
    Authors: Alharris Et al.
    Oncotarget  2019;10:45
  9. Cannabinoid Receptor 1 Blockade Attenuates Obesity and Adipose Tissue Type 1 Inflammation Through miR-30e-5p Regulation of Delta-Like-4 in Macrophages and Consequently Downregulation of Th1 Cells.
    Authors: Miranda Et al.
    Front Immunol  2019;10:1049
  10. OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons.
    Authors: Xiao Et al.
    Elife  2018;7
  11. Activity in nodose ganglia neurons after treatment with CP 55,940 and cholecystokinin.
    Authors: Johnston Et al.
    Physiol Rep  2018;6:e13927
  12. Selective Role of RGS9-2 in Regulating Retrograde Synaptic Signaling of Indirect Pathway Medium Spiny Neurons in Dorsal Striatum.
    Authors: Song Et al.
    J Neurosci  2018;38:7120
  13. Ca2+ Signaling and IL-8 Secretion in Human Testicular Peritubular Cells Involve the Cation Channel TRPV2.
    Authors: Eubler Et al.
    Int J Mol Sci  2018;19
  14. Input-Timing-Dependent Plasticity in the Hippocampal CA2 Region and Its Potential Role in Social Memory.
    Authors: Leroy Et al.
    Neuron  2017;95:1089
  15. Involvement of cannabinoid system in the nucleus accumbens on delay-based decision making in the rat.
    Authors: Fatahi
    Behav Brain Res.  2017;337:107
  16. Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
    Authors: Han
    Brain Res  2017;1663:132
  17. AM404, paracetamol metabolite, prevents prostaglandin synthesis in activated microglia by inhibiting COX activity.
    Authors: Saliba
    J Neuroinflammation  2017;14(1):246
  18. AMPK contributes to aerobic exercise-induced antinociception downstream of endocannabinoids.
    Authors: King-Himmelreich
    Neuropharmacology  2017;124:134
  19. Orphan nuclear receptor ERRγ is a key regulator of human fibrinogen gene expression.
    Authors: Zhang
    PLoS One  2017;12(7):e0182141
  20. Dentate cannabinoid-sensitive interneurons undergo unique and selective strengthening of mutual synaptic inhibition in experimental epilepsy.
    Authors: Yu Et al.
    Neurobiol Dis  2016;89:23
  21. Up-regulation of immunomodulatory effects of mouse bone-marrow derived mesenchymal stem cells by tetrahydrocannabinol pre-treatment involving cannabinoid receptor CB2.
    Authors: Xie Et al.
    Oncotarget  2016;7:6436
  22. Endocannabinoid dynamics gate spike-timing dependent depression and potentiation.
    Authors: Cui Et al.
    Elife  2016;5:e13185
  23. Abnormal cannabidiol attenuates experimental colitis in mice, promotes wound healing and inhibits neutrophil recruitment.
    Authors: Krohn Et al.
    J Inflamm (Lond)  2016;13:21
  24. Impaired Excitatory Neurotransmission in the Urinary Bladder from the Obese Zucker Rat: Role of Cannabinoid Receptors.
    Authors: Blaha Et al.
    PLoS One  2016;11:e0157424
  25. Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors
    Authors: Shang Et al.
    Biochemical Pharmacology  2016;
  26. Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex.
    Authors: Martin Et al.
    Br J Pharmacol  2015;9:457
  27. Tonic endocannabinoid-mediated modulation of GABA release is independent of the CB1 content of axon terminals.
    Authors: Lenkey Et al.
    Sci Rep  2015;6:6557
  28. FAAH genetic variation enhances fronto-amygdala function in mouse and human.
    Authors: Dincheva Et al.
    Nat Commun  2015;6:6395
  29. Regional effects of endocannabinoid, BDNF and FGF receptor signalling on neuroblast motility and guidance along the rostral migratory stream.
    Authors: Zhou Et al.
    Nat Commun  2015;64:32
  30. Role of the endocannabinoid system in obesity induced by neuropeptide Y overexpression in noradrenergic neurons.
    Authors: Vähätalo Et al.
    Mol Cell Neurosci  2015;5:e151
  31. Differential immune mechanism to HIV-1 Tat variants and its regulation by AEA [corrected].
    Authors: Krishnan and Chatterjee
    PLoS One  2015;5:9887
  32. Involvement of GluR2 up-regulation in neuroprotection by electroacupuncture pretreatment via cannabinoid CB1 receptor in mice.
    Authors: Liu Et al.
    Nutr Diabetes  2015;5:9490
  33. Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments.
    Authors: Stornaiuolo Et al.
    Sci Rep  2015;5:15453
  34. Mitochondrial CB1 receptor is involved in ACEA-induced protective effects on neurons and mitochondrial functions.
    Authors: Ma Et al.
    Sci Rep  2015;5:12440
  35. Coadministration of indomet. and MinCyc attenuates established PacT.-induced neuropathic thermal hyperalgesia: Involvement of cannabinoid CB1 receptors.
    Authors: Parvathy and Masocha
    J Neurosci  2015;5:10541
  36. Activation of cannabinoid receptor 1 inhibits increased bladder activity induced by nerve growth factor.
    Authors: Wang Et al.
    Neurosci Lett  2015;589:19
  37. Cannabinoid receptor CB2 is involved in tetrahydrocannabinol-induced anti-inflammation against lipopolysaccharide in MG-63 cells.
    Authors: Yang Et al.
    Sci Rep  2015;2015:362126
  38. Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures.
    Authors: Malek Et al.
    Neural Plast  2015;2015:130639
  39. Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation.
    Authors: Bashashati Et al.
    Br J Pharmacol  2015;172:3099
  40. A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome.
    Authors: Bowles Et al.
    Mol Pharmacol  2015;112:285
  41. Pharmacological Blockade of Cannabinoid CB1 Receptors in Diet-Induced Obesity Regulates Mitochondrial Dihydrolipoamide Dehydrogenase in Muscle.
    Authors: Arrabal Et al.
    PLoS One  2015;10:e0145244
  42. Anoctamin Calcium-Activated Chloride Channels May Modulate Inhibitory Transmission in the Cerebellar Cortex.
    Authors: Zhang Et al.
    PLoS One  2015;10:e0142160
  43. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    Proc Natl Acad Sci U S A  2015;10:e0136546
  44. Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
    Authors: Stanley Et al.
    Front Cell Neurosci  2015;107:568
  45. Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
    Authors: Alpár Et al.
    J Neurosci  2014;5:4421
  46. Presynaptic calcium channel inhibition underlies CB1 cannabinoid receptor-mediated suppression of GABA release.
    Authors: Szabó Et al.
    Mediators Inflamm  2014;34:7958
  47. Hippocampal metaplasticity is required for the formation of temporal associative memories.
    Authors: Xu Et al.
    J Neurosci  2014;34:16762
  48. Miswiring the brain: △9-tetrahydrocannabinol disrupts cortical development by inducing an SCG10/stathmin-2 degradation pathway.
    Authors: Tortoriello Et al.
    Proc Natl Acad Sci U S A  2014;33:668
  49. CB1 cannabinoid receptor stimulation during adolescence impairs the maturation of GABA function in the adult rat prefrontal cortex.
    Authors: Cass Et al.
    Mol Psychiatry  2014;19:536
  50. CB1 cannabinoid receptors are involved in neuroleptic-induced enhancement of brain neurotensin.
    Authors: Hassanzadeh and Rostami
    J Neurosci  2014;17:181
  51. Effects of the endogenous cannabinoid anandamide on voltage-dependent sodium and calcium channels in rat ventricular myocytes.
    Authors: Kury Et al.
    Br J Pharmacol  2014;171:3485
  52. 2-arachidonoylglycerol effects in cytotrophoblasts: metabolic enzymes expression and apoptosis in BeWo cells.
    Authors: Costa Et al.
    Reproduction  2014;147:301
  53. Expression and functional relevance of cannabinoid receptor 1 in Hodgkin lymphoma.
    Authors: Benz Et al.
    PLoS One  2013;8:e81675
  54. The cannabinoid receptor type 2 as mediator of mesenchymal stromal cell immunosuppressive properties.
    Authors: Rossi Et al.
    PLoS One  2013;8:e80022
  55. Hepatic cannabinoid receptor type 1 mediates alcohol-induced regulation of bile acid enzyme genes expression via CREBH.
    Authors: Chanda Et al.
    PLoS One  2013;8:e68845
  56. Cannabinoid HU210 protects isolated rat stomach against impairment caused by serum of rats with experimental acute pancreatitis.
    Authors: Cao Et al.
    PLoS One  2013;7:e52921
  57. The cannabinoid δ(9)-tetrahydrocannabivarin (THCV) ameliorates Ins sensitivity in two mouse models of obesity.
    Authors: Wargent Et al.
    Nutr Diabetes  2013;3:e68
  58. Diacylglycerol lipase α manipulation reveals developmental roles for intercellular endocannabinoid signaling.
    Authors: Keimpema Et al.
    Nat Commun  2013;3:2093
  59. Cannabinoids ameliorate impairments induced by chronic stress to synaptic plasticity and short-term memory.
    Authors: Abush and Akirav
    Neuropsychopharmacology  2013;38:1521
  60. Cannabinoid 1 receptors are critical for the innate immune response to TLR4 stimulation.
    Authors: Duncan Et al.
    Am J Physiol Regul Integr Comp Physiol  2013;305:R224
  61. CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release.
    Authors: Malenczyk Et al.
    J Biol Chem  2013;288:32685
  62. Inhibition of fatty acid amide hydrolase activates Nrf2 signalling and induces heme oxygenase 1 transcription in breast cancer cells.
    Authors: Li Et al.
    Br J Pharmacol  2013;170:489
  63. Gene-environment interactions affect long-term depression (LTD) through changes in DA receptor affinity in Snap25 deficient mice.
    Authors: Baca Et al.
    Brain Res  2013;1532:85
  64. Working memory- and anxiety-related behavioral effects of repeated nicotine as a stressor: the role of cannabinoid receptors.
    Authors: Hayase
    BMC Neurosci  2013;14:20
  65. The cannabinoid WIN 55,212-2 decreases specificity protein transcription factors and the oncogenic cap protein eIF4E in colon cancer cells.
    Authors: Sreevalsan and Safe
    Mol Cancer Ther  2013;12:2483
  66. Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection.
    Authors: Guida Et al.
    Mol Pain  2012;8:60
  67. Monohydroxylated metabolites of the K2 synthetic cannabinoid JWH-073 retain intermediate to high cannabinoid 1 receptor (CB1R) affinity and exhibit neutral antagonist to partial agonist activity.
    Authors: Brents Et al.
    Biochem Pharmacol  2012;83:952
  68. Regulation of MMP-9 by a WIN-binding site in the monocyte-macrophage system independent from cannabinoid receptors.
    Authors: Tauber Et al.
    PLoS One  2012;7:e48272
  69. CB1 receptor autoradiographic characterization of the individual differences in approach and avoidance motivation.
    Authors: Laricchiuta Et al.
    PLoS One  2012;7:e42111
  70. A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation.
    Authors: Tozzi Et al.
    PLoS One  2012;7:e38312
  71. Differences in spontaneously avoiding or approaching mice reflect differences in CB1-mediated signaling of dorsal striatal transmission.
    Authors: Laricchiuta Et al.
    PLoS One  2012;7:e33260
  72. A Role for the Cannabinoid 1 Receptor in Neuronal Differentiation of Adult Spinal Cord Progenitors in vitro is Revealed through Pharmacological Inhibition and Genetic Deletion.
    Authors: Sideris Et al.
    Front Neurosci  2012;6:4
  73. Nicotine-induced anxiety-like behavior in a rat model of the novelty-seeking phenotype is associated with long-lasting neuropeptidergic and neuroplastic adaptations in the amygdala: effects of the cannabinoid receptor 1 antagonist AM251.
    Authors: Aydin Et al.
    Neuropharmacology  2012;63:1335
  74. Opposing roles for cannabinoid receptor type-1 (CB1) and transient receptor potential vanilloid type-1 channel (TRPV1) on the modulation of panic-like responses in rats.
    Authors: Casarotto Et al.
    Pain  2012;37:478
  75. Cannabinoids prevent the development of behavioral and endocrine alterations in a rat model of intense stress.
    Authors: Ganon-Elazar and Akirav
    Neuropsychopharmacology  2012;37:456
  76. On disruption of fear memory by reconsolidation blockade: evidence from cannabidiol treatment.
    Authors: Stern Et al.
    Neuropsychopharmacology  2012;37:2132
  77. Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons.
    Authors: Peterfi Et al.
    J Neurosci  2012;32:14448
  78. Tonic and transient endocannabinoid regulation of AMPAergic miniature postsynaptic currents and homeostatic plasticity in embryonic motor networks.
    Authors: Gonzalez-Islas Et al.
    Sci Rep  2012;32:13597
  79. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
    Authors: Caiati Et al.
    Sci Rep  2012;2:285
  80. Activation of cannabinoid receptor type 1 (Cb1r) disrupts hepatic Ins receptor signaling via cyclic AMP-response element-binding protein H (Crebh)-mediated induction of Lipin1 gene.
    Authors: Chanda Et al.
    Br J Pharmacol  2012;287:38041
  81. Repeated mor. treatment-mediated hyperalgesia, allodynia and spinal glial activation are blocked by co-administration of a selective cannabinoid receptor type-2 agonist.
    Authors: Tumati Et al.
    J Neuroimmunol  2012;244:23
  82. TRPV1-dependent and -independent alterations in the limbic cortex of neuropathic mice: impact on glial caspases and pain perception.
    Authors: Giordano Et al.
    Cereb Cortex  2012;22:2495
  83. The endocannabinoid system modulates the valence of the emotion associated to food ingestion.
    Authors: Méndez-D?az Et al.
    Addict Biol  2012;17:725
  84. Cannabinoid CB(2) receptor attenuates morphine-induced inflammatory responses in activated microglial cells.
    Authors: Merighi Et al.
    Br J Pharmacol  2012;166:2371
  85. The cannabinoid CB1 receptor antagonists rim. (SR141716) and AM251 directly potentiate GABA(A) receptors.
    Authors: Baur Et al.
    Br J Pharmacol  2012;165:2479
  86. Cannabinoid CB(2) receptors modulate ERK-1/2 kinase signalling and NO release in microglial cells stimulated with bacterial lipopolysaccharide.
    Authors: Merighi Et al.
    Br J Pharmacol  2012;165:1773
  87. Effects of gonadal hormones on the peripheral cannabinoid receptor 1 (CB1R) system under a myositis condition in rats.
    Authors: Niu Et al.
    J Pharmacol Exp Ther  2012;153:2283
  88. The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action.
    Authors: Hamtiaux Et al.
    BMC Cancer  2012;12:92
  89. Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer.
    Authors: Liu Et al.
    Mol Cancer Ther  2012;11:1421
  90. The blockade of the transient receptor potential vanilloid type 1 and fatty acid amide hydrolase decreases symptoms and central sequelae in the medial prefrontal cortex of neuropathic rats.
    Authors: Novellis Et al.
    Mol Pain  2011;7:7
  91. Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism.
    Authors: Hamtiaux Et al.
    PLoS One  2011;6:e26823
  92. The antinociceptive effects of JWH-015 in chronic inflammatory pain are produced by nitric oxide-cGMP-PKG-KATP pathway activation mediated by opioids.
    Authors: Negrete Et al.
    PLoS One  2011;6:e26688
  93. Acute overactive endocannabinoid signaling induces glucose intolerance, hepatic steatosis, and novel cannabinoid receptor 1 responsive genes.
    Authors: Ruby Et al.
    PLoS One  2011;6:e26415
  94. Phase I hydroxylated metabolites of the K2 synthetic cannabinoid JWH-018 retain in vitro and in vivo cannabinoid 1 receptor affinity and activity.
    Authors: Brents Et al.
    PLoS One  2011;6:e21917
  95. Expression of the cannabinoid system in muscle: effects of a high-fat diet and CB1 receptor blockade.
    Authors: Crespillo Et al.
    Biochem J  2011;433:175
  96. Regulation of hippocampal cannabinoid CB1 receptor actions by adenosine A1 receptors and chronic caffeine administration: implications for the effects of δ9-tetrahydrocannabinol on spatial memory.
    Authors: Sousa Et al.
    Neuropsychopharmacology  2011;36:472
  97. Alterations of endocannabinoid signaling, synaptic plasticity, learning, and memory in monoacylglycerol lipase knock-out mice.
    Authors: Pan Et al.
    J Cell Biol  2011;31:13420
  98. Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms.
    Authors: Li and Burrell
    Learn Mem  2011;18:545
  99. Differential effects of cannabinoid receptor agonist on social discrimination and contextual fear in amygdala and hippocampus.
    Authors: Segev and Akirav
    Learn Mem  2011;18:254
  100. The Role of the Endocannabinoids in Suppression of the Hypothalamic-pituitary-adrenal Axis Activity by dox.
    Authors: Hassanzadeh and Hassanzadeh
    J Leukoc Biol  2011;14:414
  101. Cannabinoid CB1 receptor antagonism prevents neurochemical and behavioural deficits induced by chronic phencyclidine.
    Authors: Guidali Et al.
    Int J Neuropsychopharmacol  2011;14:17
  102. Post-ictal analgesia in genetically epilepsy-prone rats is induced by audiogenic seizures and involves cannabinoid receptors in the periaqueductal gray.
    Authors: Samineni Et al.
    Brain Res  2011;1389:177
  103. Endocannabinoids mediate synaptic plasticity at glutamatergic synapses on spiny neurons within a basal ganglia nucleus necessary for song learning.
    Authors: Thompson and Perkel
    J Neurophysiol  2011;105:1159
  104. The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period.
    Authors: Jiang Et al.
    Neuron  2010;66:248
  105. THC Prevents MDMA Neurotoxicity in Mice.
    Authors: Touriño Et al.
    PLoS One  2010;5:e9143
  106. The cannabinoid WIN55,212-2 protects against oxidized LDL-induced inflammatory response in murine macrophages.
    Authors: Hao Et al.
    Iran J Basic Med Sci  2010;51:2181
  107. Cannabidiol displays antiepileptiform and antiseizure properties in vitro and in vivo.
    Authors: Jones Et al.
    Cereb Cortex  2010;332:569
  108. A putative 'pre-nervous' endocannabinoid system in early echinoderm development.
    Authors: Buznikov Et al.
    Dev Neurosci  2010;32:1
  109. 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
  110. 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
  111. A refractory period for rejuvenating GABAergic synaptic transmission and ocular dominance plasticity with dark exposure.
    Authors: Huang Et al.
    J Neurosci  2010;30:16636
  112. Repeated stress impairs endocannabinoid signaling in the paraventricular nucleus of the hypothalamus.
    Authors: Wamsteeker Et al.
    J Neurosci  2010;30:11188
  113. Cannabinoids excite circadian clock neurons.
    Authors: Acuna-Goycolea Et al.
    J Neurosci  2010;30:10061
  114. Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy.
    Authors: Bhaskaran and Smith
    Endocrinology  2010;223:529
  115. Inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in hypertension without adverse metabolic effects.
    Authors: Godlewski Et al.
    Chem Biol  2010;17:1256
  116. Interaction between anandamide and sphingosine-1-phosphate in mediating vasorelaxation in rat coronary artery.
    Authors: Mair Et al.
    Br J Pharmacol  2010;161:176
  117. Endocannabinoid modulation of hyperaemia evoked by physiologically relevant stimuli in the rat primary somatosensory cortex.
    Authors: Ho Et al.
    Neuropsychopharmacology  2010;160:736
  118. GPR55 ligands promote receptor coupling to multiple signalling pathways.
    Authors: Henstridge Et al.
    Br J Pharmacol  2010;160:604
  119. Spinal and peripheral analgesic effects of the CB2 cannabinoid receptor agonist AM1241 in two models of bone cancer-induced pain.
    Authors: Curto-Reyes Et al.
    Br J Pharmacol  2010;160:561
  120. Retrograde endocannabinoid signaling reduces GABAergic synaptic transmission to gonadotropin-releasing hormone neurons.
    Authors: Farkas Et al.
    J Biol Chem  2010;151:5818
  121. Regulation of the hypothalamic-pituitary-adrenal axis circadian rhythm by endocannabinoids is sexually diergic.
    Authors: Atkinson Et al.
    Endocrinology  2010;151:3720
  122. Network mechanisms of theta related neuronal activity in hippocampal CA1 pyramidal neurons.
    Authors: Losonczy Et al.
    Nat Neurosci  2010;13:967
  123. Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system.
    Authors: Schlosburg Et al.
    Nat Neurosci  2010;13:1113
  124. Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor.
    Authors: Yuan and Burrell
    J Neurophysiol  2010;104:2766
  125. Gz mediates the long-lasting desensitization of brain CB1 receptors and is essential for cross-tolerance with mor.
    Authors: Garzón Et al.
    Mol Pain  2009;5:11
  126. PKCε regulates behavioral sensitivity, binding and tolerance to the CB1 receptor agonist WIN55,212-2.
    Authors: Wallace Et al.
    Iran J Basic Med Sci  2009;34:1733
  127. The neuroprotective impact of the leak potassium channel TASK1 on stroke development in mice.
    Authors: Meuth Et al.
    Exp Neurol  2009;33:42675
  128. Blockade of 2-arachidonoylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) Enhances retrograde endocannabinoid signaling.
    Authors: Pan Et al.
    J Pharmacol Exp Ther  2009;331:591
  129. Central antinociception induced by mu-opioid receptor agonist morphine, but not delta- or kappa-, is mediated by cannabinoid CB1 receptor.
    Authors: Pacheco Et al.
    Br J Pharmacol  2009;158:225
  130. Effect of the CB(1) receptor antagonists rim. and AM251 on the firing rate of dorsal raphe nucleus neurons in rat brain slices.
    Authors: Mendiguren and Pineda
    Br J Pharmacol  2009;158:1579
  131. Endogenous cannabinoids induce fever through the activation of CB1 receptors.
    Authors: Fraga Et al.
    Neuropsychopharmacology  2009;157:1494
  132. Acute hypertension reveals depressor and vasodilator effects of cannabinoids in conscious rats.
    Authors: Ho and Gardiner
    Br J Pharmacol  2009;156:94
  133. Processing cardiovascular information in the vlPAG during electroacupuncture in rats: roles of endocannabinoids and GABA.
    Authors: Tjen-A-Looi Et al.
    J Appl Physiol (1985)  2009;106:1793
  134. Altered GABAergic neurotransmission is associated with increased kainate-induced seizure in prostaglandin-endoperoxide synthase-2 deficient mice.
    Authors: Toscano Et al.
    Brain Res Bull  2008;75:598
  135. Analysis of promoter regions regulating basal and interleukin-4-inducible expression of the human CB1 receptor gene in T lymphocytes.
    Authors: Börner Et al.
    Eur J Pharmacol  2008;73:1013
  136. Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling.
    Authors: Georgieva Et al.
    Br J Pharmacol  2008;581:19
  137. TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons.
    Authors: Gibson Et al.
    Neuron  2008;57:746
  138. Repeated cannabinoid injections into the rat periaqueductal gray enhance subsequent mor. antinociception.
    Authors: Wilson Et al.
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CB1R antagonist AM251 (5 µM)
By Kang Peng on 09/18/2018
Species: Mouse

bath application of the CB1R antagonist AM251 (5 µM)


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