AM 251
Chemical Name: N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
Purity: ≥99%
Biological Activity
AM 251 is a 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
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
Background References
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AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies.
Seely et al.
Neuropharmacology, 2012;63:905 -
Inverse agonism and neutral antagonism at cannabinoid CB1 receptors.
Pertwee
Life Sci., 2005;76:1307 -
The orphan receptor GPR55 is a novel cannabinoid receptor.
Ryberg et al.
Br.J.Pharmacol., 2007;152:1092 -
125I-labeled AM 251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors.
Gatley et al.
Eur.J.Pharmacol., 1996;307:331 -
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
Lan et al.
J.Med.Chem., 1999;42:769 -
Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors.
Gatley et al.
Life Sci., 1997;61:191 -
AM-251 and rimon. act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies.
Seely et al.
Neuropharmacology, 2012;63:905 -
Endocannabinoids inhibit the induction of virulence in enteric pathogens.
Ellermann et al.
Cell, 2020;
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Citations for AM 251
The citations listed below are publications that use Tocris products. Selected citations for AM 251 include:
200 Citations: Showing 1 - 10
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Feeding induced by cannabinoids is mediated independently of the melanocortin system.
Authors: Sinnayah Et al.
Proc Natl Acad Sci U S A ;3:e2202
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The orexigenic effect of ghrelin is mediated through central activation of the endogenous cannabinoid system.
Authors: Kola Et al.
Br J Pharmacol ;3:e1797
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Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex.
Authors: Lafourcade Et al.
PLoS One ;2:e709
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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
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Endocannabinoids inhibit the induction of virulence in enteric pathogens.
Authors: Ellermann Et al.
Cell 2020;
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Dual mechanism of TRKB activation by anandamide through CB1 and TRPV1 receptors.
Authors: Diniz Et al.
PeerJ 2019;7:e6493
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Routing Hippocampal Information Flow through Parvalbumin Interneuron Plasticity in Area CA2.
Authors: Nasrallah Et al.
Cell Rep 2019;27:86
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Endocannabinoid Signaling Mediates Local Dendritic Coordination between Excitatory and Inhibitory Synapses.
Authors: Hu Et al.
Cell Rep 2019;27:666
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Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells.
Authors: Alharris Et al.
Oncotarget 2019;10:45
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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
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OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons.
Authors: Xiao Et al.
Elife 2018;7
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Activity in nodose ganglia neurons after treatment with CP 55,940 and cholecystokinin.
Authors: Johnston Et al.
Physiol Rep 2018;6:e13927
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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
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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
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Input-Timing-Dependent Plasticity in the Hippocampal CA2 Region and Its Potential Role in Social Memory.
Authors: Leroy Et al.
Neuron 2017;95:1089
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Involvement of cannabinoid system in the nucleus accumbens on delay-based decision making in the rat.
Authors: Fatahi
Behav Brain Res. 2017;337:107
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Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
Authors: Han
Brain Res 2017;1663:132
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AM404, paracetamol metabolite, prevents prostaglandin synthesis in activated microglia by inhibiting COX activity.
Authors: Saliba
J Neuroinflammation 2017;14(1):246
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AMPK contributes to aerobic exercise-induced antinociception downstream of endocannabinoids.
Authors: King-Himmelreich
Neuropharmacology 2017;124:134
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Orphan nuclear receptor ERRγ is a key regulator of human fibrinogen gene expression.
Authors: Zhang
PLoS One 2017;12(7):e0182141
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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
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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
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Endocannabinoid dynamics gate spike-timing dependent depression and potentiation.
Authors: Cui Et al.
Elife 2016;5:e13185
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Abnormal cannabidiol attenuates experimental colitis in mice, promotes wound healing and inhibits neutrophil recruitment.
Authors: Krohn Et al.
J Inflamm (Lond) 2016;13:21
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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
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Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors
Authors: Shang Et al.
Biochemical Pharmacology 2016;
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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
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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
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FAAH genetic variation enhances fronto-amygdala function in mouse and human.
Authors: Dincheva Et al.
Nat Commun 2015;6:6395
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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
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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
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Differential immune mechanism to HIV-1 Tat variants and its regulation by AEA [corrected].
Authors: Krishnan and Chatterjee
PLoS One 2015;5:9887
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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
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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
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Mitochondrial CB1 receptor is involved in ACEA-induced protective effects on neurons and mitochondrial functions.
Authors: Ma Et al.
Sci Rep 2015;5:12440
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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
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Activation of cannabinoid receptor 1 inhibits increased bladder activity induced by nerve growth factor.
Authors: Wang Et al.
Neurosci Lett 2015;589:19
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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
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Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures.
Authors: Malek Et al.
Neural Plast 2015;2015:130639
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Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation.
Authors: Bashashati Et al.
Br J Pharmacol 2015;172:3099
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A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome.
Authors: Bowles Et al.
Mol Pharmacol 2015;112:285
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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
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Anoctamin Calcium-Activated Chloride Channels May Modulate Inhibitory Transmission in the Cerebellar Cortex.
Authors: Zhang Et al.
PLoS One 2015;10:e0142160
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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
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Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
Authors: Stanley Et al.
Front Cell Neurosci 2015;107:568
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Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
Authors: Alpár Et al.
J Neurosci 2014;5:4421
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Presynaptic calcium channel inhibition underlies CB1 cannabinoid receptor-mediated suppression of GABA release.
Authors: Szabó Et al.
Mediators Inflamm 2014;34:7958
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Hippocampal metaplasticity is required for the formation of temporal associative memories.
Authors: Xu Et al.
J Neurosci 2014;34:16762
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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
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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
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CB1 cannabinoid receptors are involved in neuroleptic-induced enhancement of brain neurotensin.
Authors: Hassanzadeh and Rostami
J Neurosci 2014;17:181
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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
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2-arachidonoylglycerol effects in cytotrophoblasts: metabolic enzymes expression and apoptosis in BeWo cells.
Authors: Costa Et al.
Reproduction 2014;147:301
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Expression and functional relevance of cannabinoid receptor 1 in Hodgkin lymphoma.
Authors: Benz Et al.
PLoS One 2013;8:e81675
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The cannabinoid receptor type 2 as mediator of mesenchymal stromal cell immunosuppressive properties.
Authors: Rossi Et al.
PLoS One 2013;8:e80022
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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
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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
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The cannabinoid δ(9)-tetrahydrocannabivarin (THCV) ameliorates Ins sensitivity in two mouse models of obesity.
Authors: Wargent Et al.
Nutr Diabetes 2013;3:e68
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Diacylglycerol lipase α manipulation reveals developmental roles for intercellular endocannabinoid signaling.
Authors: Keimpema Et al.
Nat Commun 2013;3:2093
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Cannabinoids ameliorate impairments induced by chronic stress to synaptic plasticity and short-term memory.
Authors: Abush and Akirav
Neuropsychopharmacology 2013;38:1521
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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
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CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release.
Authors: Malenczyk Et al.
J Biol Chem 2013;288:32685
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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
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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
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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
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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
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Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection.
Authors: Guida Et al.
Mol Pain 2012;8:60
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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
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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
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CB1 receptor autoradiographic characterization of the individual differences in approach and avoidance motivation.
Authors: Laricchiuta Et al.
PLoS One 2012;7:e42111
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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
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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
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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
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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
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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
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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
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On disruption of fear memory by reconsolidation blockade: evidence from cannabidiol treatment.
Authors: Stern Et al.
Neuropsychopharmacology 2012;37:2132
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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
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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
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Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
Authors: Caiati Et al.
Sci Rep 2012;2:285
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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
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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
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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
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The endocannabinoid system modulates the valence of the emotion associated to food ingestion.
Authors: Méndez-D?az Et al.
Addict Biol 2012;17:725
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Cannabinoid CB(2) receptor attenuates morphine-induced inflammatory responses in activated microglial cells.
Authors: Merighi Et al.
Br J Pharmacol 2012;166:2371
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The cannabinoid CB1 receptor antagonists rim. (SR141716) and AM251 directly potentiate GABA(A) receptors.
Authors: Baur Et al.
Br J Pharmacol 2012;165:2479
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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
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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
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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
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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
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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
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Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism.
Authors: Hamtiaux Et al.
PLoS One 2011;6:e26823
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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
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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
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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
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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
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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
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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
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Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms.
Authors: Li and Burrell
Learn Mem 2011;18:545
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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
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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
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Cannabinoid CB1 receptor antagonism prevents neurochemical and behavioural deficits induced by chronic phencyclidine.
Authors: Guidali Et al.
Int J Neuropsychopharmacol 2011;14:17
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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
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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
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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
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THC Prevents MDMA Neurotoxicity in Mice.
Authors: Touriño Et al.
PLoS One 2010;5:e9143
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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
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Cannabidiol displays antiepileptiform and antiseizure properties in vitro and in vivo.
Authors: Jones Et al.
Cereb Cortex 2010;332:569
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A putative 'pre-nervous' endocannabinoid system in early echinoderm development.
Authors: Buznikov Et al.
Dev Neurosci 2010;32:1
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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
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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
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A refractory period for rejuvenating GABAergic synaptic transmission and ocular dominance plasticity with dark exposure.
Authors: Huang Et al.
J Neurosci 2010;30:16636
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Repeated stress impairs endocannabinoid signaling in the paraventricular nucleus of the hypothalamus.
Authors: Wamsteeker Et al.
J Neurosci 2010;30:11188
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Cannabinoids excite circadian clock neurons.
Authors: Acuna-Goycolea Et al.
J Neurosci 2010;30:10061
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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
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Inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in hypertension without adverse metabolic effects.
Authors: Godlewski Et al.
Chem Biol 2010;17:1256
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Interaction between anandamide and sphingosine-1-phosphate in mediating vasorelaxation in rat coronary artery.
Authors: Mair Et al.
Br J Pharmacol 2010;161:176
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Endocannabinoid modulation of hyperaemia evoked by physiologically relevant stimuli in the rat primary somatosensory cortex.
Authors: Ho Et al.
Neuropsychopharmacology 2010;160:736
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GPR55 ligands promote receptor coupling to multiple signalling pathways.
Authors: Henstridge Et al.
Br J Pharmacol 2010;160:604
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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
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Retrograde endocannabinoid signaling reduces GABAergic synaptic transmission to gonadotropin-releasing hormone neurons.
Authors: Farkas Et al.
J Biol Chem 2010;151:5818
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Regulation of the hypothalamic-pituitary-adrenal axis circadian rhythm by endocannabinoids is sexually diergic.
Authors: Atkinson Et al.
Endocrinology 2010;151:3720
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Network mechanisms of theta related neuronal activity in hippocampal CA1 pyramidal neurons.
Authors: Losonczy Et al.
Nat Neurosci 2010;13:967
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Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system.
Authors: Schlosburg Et al.
Nat Neurosci 2010;13:1113
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Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor.
Authors: Yuan and Burrell
J Neurophysiol 2010;104:2766
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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
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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
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The neuroprotective impact of the leak potassium channel TASK1 on stroke development in mice.
Authors: Meuth Et al.
Exp Neurol 2009;33:42675
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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
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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
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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
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Endogenous cannabinoids induce fever through the activation of CB1 receptors.
Authors: Fraga Et al.
Neuropsychopharmacology 2009;157:1494
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Acute hypertension reveals depressor and vasodilator effects of cannabinoids in conscious rats.
Authors: Ho and Gardiner
Br J Pharmacol 2009;156:94
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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
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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
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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
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Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling.
Authors: Georgieva Et al.
Br J Pharmacol 2008;581:19
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TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons.
Authors: Gibson Et al.
Neuron 2008;57:746
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Repeated cannabinoid injections into the rat periaqueductal gray enhance subsequent mor. antinociception.
Authors: Wilson Et al.
Neuropharmacology 2008;55:1219
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Cannabinoid receptor activation in the nucleus tractus solitaries produces baroreflex-like responses in the rat.
Authors: Durakoglugil and Orer
Int J Biomed Sci 2008;4:229
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Dichotomous DArgic control of striatal synaptic plasticity.
Authors: Shen Et al.
Science 2008;321:848
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Roles of endocannabinoids in heterosynaptic long-term depression of excitatory synaptic transmission in visual cortex of young mice.
Authors: Huang Et al.
J Neurosci 2008;28:7074
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Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors.
Authors: Melis Et al.
J Neurosci 2008;28:13985
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Electroacupuncture of 2?hz has a rewarding effect: evidence from a conditioned place preference study in rats.
Authors: Xia Et al.
Evid Based Complement Alternat Med 2008;2011:730514
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Modulation of the anti-nociceptive effects of 2-arachidonoyl glycerol by peripherally administered FAAH and MGL inhibitors in a neuropathic pain model.
Authors: Desroches Et al.
Eur J Neurosci 2008;155:913
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Interactions between CB(1) receptors and TRPV1 channels mediated by 12-HPETE are cytotoxic to mesencephalic DArgic neurons.
Authors: Kim Et al.
Br J Pharmacol 2008;155:253
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MDA7: a novel selective agonist for CB2 receptors that prevents allodynia in rat neuropathic pain models.
Authors: Naguib Et al.
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The mu-opioid receptor agonist morphine, but not agonists at delta- or kappa-opioid receptors, induces peripheral antinociception mediated by cannabinoid receptors.
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Activation of cannabinoid receptors prevents antigen-induced asthma-like reaction in guinea pigs.
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The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms.
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The differential contractile responses to capsaicin and anandamide in muscle strips isolated from the rat urinary bladder.
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Potentiation of electrical and chemical synaptic transmission mediated by endocannabinoids.
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Effects of peripheral cannabinoid receptor ligands on motility and polarization in neutrophil-like HL60 cells and human neutrophils.
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Differential effect of cannabinoid agonists and endocannabinoids on histamine release from distinct regions of the rat brain.
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Anandamide mediates hyperdynamic circulation in cirrhotic rats via CB(1) and VR(1) receptors.
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Modulation of P-glycoprotein activity by cannabinoid molecules in HK-2 renal cells.
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Effects of intra-amygdala infusion of CB1 receptor agonists on the reconsolidation of fear-potentiated startle.
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Amnestic effect of intrahippocampal AM251, a CB1-selective blocker, in the inhibitory avoidance, but not in the open field habituation task, in rats.
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Endocannabinoids control the induction of cerebellar LTD.
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The wake-promoting peptide orexin-B inhibits glutamatergic transmission to dorsal raphe nucleus serotonin neurons through retrograde endocannabinoid signaling.
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Species and strain differences in the expression of a novel glutamate-modulating cannabinoid receptor in the rodent hippocampus.
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Anandamide acts as a vasodilator of dural blood vessels in vivo by activating TRPV1 receptors.
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Effects of cannabinoid receptor-2 activation on accelerated gastrointestinal transit in lipopolysaccharide-treated rats.
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Endocannabinoids acting at cannabinoid-1 receptors regulate cardiovascular function in hypertension.
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The inhibitory effect of anandamide on luteinizing hormone-releasing hormone secretion is reversed by estrogen.
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The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response.
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Evidence of a novel site mediating anandamide-induced negative inotropic and coronary vasodilatator responses in rat isolated hearts.
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Despite substantial degradation, 2-arachidonoylglycerol is a potent full efficacy agonist mediating CB(1) receptor-dependent G-protein activation in rat cerebellar membranes.
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Br J Pharmacol 2001;134:664
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Identification of two distinct vasodilator pathways activated by ATP in the mesenteric bed of the rat.
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