AM 251

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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% (HPLC)
Citations (200)
Reviews (1)
Literature (2)

Biological Activity for AM 251

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 for AM 251

M. Wt 555.24
Formula C22H21Cl2IN4O
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 183232-66-8
PubChem ID 2125
Smiles CC1=C(N(N=C1C(=O)NN1CCCCC1)C1=C(Cl)C=C(Cl)C=C1)C1=CC=C(I)C=C1

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.

Solubility Data for AM 251

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 13.88 25
DMSO 55.52 100

Preparing Stock Solutions for AM 251

The following data is based on the product molecular weight 555.24. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.8 mL 9.01 mL 18.01 mL
5 mM 0.36 mL 1.8 mL 3.6 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets for AM 251

Certificate of Analysis / Product Datasheet
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References for AM 251

References are publications that support the biological activity of the product.

Gatley et al (1996) 125I-labeled AM 251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors. Eur.J.Pharmacol. 307 331 PMID: 8836622

Lan et al (1999) Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J.Med.Chem. 42 769 PMID: 10052983

Pertwee (2005) Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci. 76 1307 PMID: 15670612

Gatley et al (1997) Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors. Life Sci. 61 191 PMID: 9335234

Ryberg et al (2007) The orphan receptor GPR55 is a novel cannabinoid receptor. Br.J.Pharmacol. 152 1092 PMID: 17876302

Seely et al (2012) AM-251 and rimon. act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies. Neuropharmacology 63 905 PMID: 22771770

Ellermann et al (2020) Endocannabinoids inhibit the induction of virulence in enteric pathogens. Cell 183 650 PMID: 33031742

If you know of a relevant reference for AM 251, please let us know.

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Keywords: AM 251, AM 251 supplier, Potent, CB1, antagonist, GPR55, agonist, cannabinoid, receptors, AM251, cb1r, Receptors, 1117, Tocris Bioscience

200 Citations for AM 251

Citations are publications that use Tocris products. Selected citations for AM 251 include:

Miranda et al (2019) 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. Front Immunol 10 1049 PMID: 31134094

Hu et al (2019) Endocannabinoid Signaling Mediates Local Dendritic Coordination between Excitatory and Inhibitory Synapses. Cell Rep 27 666 PMID: 30995465

Nasrallah et al (2019) Routing Hippocampal Information Flow through Parvalbumin Interneuron Plasticity in Area CA2. Cell Rep 27 86 PMID: 30943417

Li et al (2013) Inhibition of fatty acid amide hydrolase activates Nrf2 signalling and induces heme oxygenase 1 transcription in breast cancer cells. Br J Pharmacol 170 489 PMID: 23347118

Duncan et al (2013) Cannabinoid 1 receptors are critical for the innate immune response to TLR4 stimulation. Am J Physiol Regul Integr Comp Physiol 305 R224 PMID: 23739343

Hayase (2013) Working memory- and anxiety-related behavioral effects of repeated nicotine as a stressor: the role of cannabinoid receptors. BMC Neurosci 14 20 PMID: 23394117

Baca et al (2013) Gene-environment interactions affect long-term depression (LTD) through changes in DA receptor affinity in Snap25 deficient mice. Brain Res 1532 85 PMID: 23939223

Sideris et al (2012) 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. Front Neurosci 6 4 PMID: 22291615

Tauber et al (2012) Regulation of MMP-9 by a WIN-binding site in the monocyte-macrophage system independent from cannabinoid receptors. PLoS One 7 e48272 PMID: 23139770

Giordano et al (2012) TRPV1-dependent and -independent alterations in the limbic cortex of neuropathic mice: impact on glial caspases and pain perception. Cereb Cortex 22 2495 PMID: 22139792

Laricchiuta et al (2012) Differences in spontaneously avoiding or approaching mice reflect differences in CB1-mediated signaling of dorsal striatal transmission. PLoS One 7 e33260 PMID: 22413007

Merighi et al (2012) Cannabinoid CB(2) receptors modulate ERK-1/2 kinase signalling and NO release in microglial cells stimulated with bacterial lipopolysaccharide. Br J Pharmacol 165 1773 PMID: 21951063

Peterfi et al (2012) Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons. J Neurosci 32 14448 PMID: 23055515

Buznikov et al (2010) A putative 'pre-nervous' endocannabinoid system in early echinoderm development. Dev Neurosci 32 1 PMID: 19907129

Mair et al (2010) Interaction between anandamide and sphingosine-1-phosphate in mediating vasorelaxation in rat coronary artery. Br J Pharmacol 161 176 PMID: 20718749

Jiang et al (2010) The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period. Neuron 66 248 PMID: 20435001

Yuan and Burrell (2010) Endocannabinoid-dependent LTD in a nociceptive synapse requires activation of a presynaptic TRPV-like receptor. J Neurophysiol 104 2766 PMID: 20884761

Atkinson et al (2010) Regulation of the hypothalamic-pituitary-adrenal axis circadian rhythm by endocannabinoids is sexually diergic. Endocrinology 151 3720 PMID: 20534730

Schlosburg et al (2010) Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system. Nat Neurosci 13 1113 PMID: 20729846

Henstridge et al (2010) GPR55 ligands promote receptor coupling to multiple signalling pathways. Br J Pharmacol 160 604 PMID: 20136841

Curto-Reyes et al (2010) Spinal and peripheral analgesic effects of the CB2 cannabinoid receptor agonist AM1241 in two models of bone cancer-induced pain. Br J Pharmacol 160 561 PMID: 20233215

Song et al (2018) Selective Role of RGS9-2 in Regulating Retrograde Synaptic Signaling of Indirect Pathway Medium Spiny Neurons in Dorsal Striatum. J Neurosci 38 7120 PMID: 30006367

Krohn et al (2016) Abnormal cannabidiol attenuates experimental colitis in mice, promotes wound healing and inhibits neutrophil recruitment. J Inflamm (Lond) 13 21 PMID: 27418880

Cui et al (2016) Endocannabinoid dynamics gate spike-timing dependent depression and potentiation. Elife 5 e13185 PMID: 26920222

Blaha et al (2016) Impaired Excitatory Neurotransmission in the Urinary Bladder from the Obese Zucker Rat: Role of Cannabinoid Receptors. PLoS One 11 e0157424 PMID: 27285468

Yang et al (2015) Cannabinoid receptor CB2 is involved in tetrahydrocannabinol-induced anti-inflammation against lipopolysaccharide in MG-63 cells. Sci Rep 2015 362126 PMID: 25653478

Liu et al (2015) Involvement of GluR2 up-regulation in neuroprotection by electroacupuncture pretreatment via cannabinoid CB1 receptor in mice. Nutr Diabetes 5 9490 PMID: 25830356

Vähätalo et al (2015) Role of the endocannabinoid system in obesity induced by neuropeptide Y overexpression in noradrenergic neurons. Mol Cell Neurosci 5 e151 PMID: 25915740

Zhou et al (2015) Regional effects of endocannabinoid, BDNF and FGF receptor signalling on neuroblast motility and guidance along the rostral migratory stream. Nat Commun 64 32 PMID: 25481343

Dincheva et al (2015) FAAH genetic variation enhances fronto-amygdala function in mouse and human. Nat Commun 6 6395 PMID: 25731744

Lenkey et al (2015) Tonic endocannabinoid-mediated modulation of GABA release is independent of the CB1 content of axon terminals. Sci Rep 6 6557 PMID: 25891347

Smith et al (2015) The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation. Proc Natl Acad Sci U S A 10 e0136546 PMID: 26414859

Bowles et al (2015) A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome. Mol Pharmacol 112 285 PMID: 25535367

Stanley et al (2015) Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation. Front Cell Neurosci 107 568 PMID: 26092099

Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Br J Pharmacol 9 457 PMID: 26648844

Rossi et al (2013) The cannabinoid receptor type 2 as mediator of mesenchymal stromal cell immunosuppressive properties. PLoS One 8 e80022 PMID: 24312195

Stern et al (2012) On disruption of fear memory by reconsolidation blockade: evidence from cannabidiol treatment. Neuropsychopharmacology 37 2132 PMID: 22549120

Tumati et al (2012) Repeated mor. treatment-mediated hyperalgesia, allodynia and spinal glial activation are blocked by co-administration of a selective cannabinoid receptor type-2 agonist. J Neuroimmunol 244 23 PMID: 22285397

Laricchiuta et al (2012) CB1 receptor autoradiographic characterization of the individual differences in approach and avoidance motivation. PLoS One 7 e42111 PMID: 22848724

Brents et al (2012) 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. Biochem Pharmacol 83 952 PMID: 22266354

Liu et al (2012) Betulinic acid targets YY1 and ErbB2 through cannabinoid receptor-dependent disruption of microRNA-27a:ZBTB10 in breast cancer. Mol Cancer Ther 11 1421 PMID: 22553354

Guida et al (2012) Salvinorin A reduces mechanical allodynia and spinal neuronal hyperexcitability induced by peripheral formalin injection. Mol Pain 8 60 PMID: 22913292

Ganon-Elazar and Akirav (2012) Cannabinoids prevent the development of behavioral and endocrine alterations in a rat model of intense stress. Neuropsychopharmacology 37 456 PMID: 21918506

Tozzi et al (2012) A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation. PLoS One 7 e38312 PMID: 22715379

Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285 PMID: 22368777

Jones et al (2010) Cannabidiol displays antiepileptiform and antiseizure properties in vitro and in vivo. Cereb Cortex 332 569 PMID: 19906779

Ho et al (2010) Endocannabinoid modulation of hyperaemia evoked by physiologically relevant stimuli in the rat primary somatosensory cortex. Neuropsychopharmacology 160 736 PMID: 20590576

Farkas et al (2010) Retrograde endocannabinoid signaling reduces GABAergic synaptic transmission to gonadotropin-releasing hormone neurons. J Biol Chem 151 5818 PMID: 20926585

Acuna-Goycolea et al (2010) Cannabinoids excite circadian clock neurons. J Neurosci 30 10061 PMID: 20668190

Hao et al (2010) The cannabinoid WIN55,212-2 protects against oxidized LDL-induced inflammatory response in murine macrophages. Iran J Basic Med Sci 51 2181 PMID: 20305287

Eubler et al (2018) Ca2+ Signaling and IL-8 Secretion in Human Testicular Peritubular Cells Involve the Cation Channel TRPV2. Int J Mol Sci 19 PMID: 30235802

Xie et al (2016) Up-regulation of immunomodulatory effects of mouse bone-marrow derived mesenchymal stem cells by tetrahydrocannabinol pre-treatment involving cannabinoid receptor CB2. Oncotarget 7 6436 PMID: 26824325

Yu et al (2016) Dentate cannabinoid-sensitive interneurons undergo unique and selective strengthening of mutual synaptic inhibition in experimental epilepsy. Neurobiol Dis 89 23 PMID: 26804027

Shang et al (2016) Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors Biochemical Pharmacology PMID: 27641813

Costa et al (2014) 2-arachidonoylglycerol effects in cytotrophoblasts: metabolic enzymes expression and apoptosis in BeWo cells. Reproduction 147 301 PMID: 24324206

Cass et al (2014) CB1 cannabinoid receptor stimulation during adolescence impairs the maturation of GABA function in the adult rat prefrontal cortex. Mol Psychiatry 19 536 PMID: 24589887

Xu et al (2014) Hippocampal metaplasticity is required for the formation of temporal associative memories. J Neurosci 34 16762 PMID: 25505329

Kury et al (2014) Effects of the endogenous cannabinoid anandamide on voltage-dependent sodium and calcium channels in rat ventricular myocytes. Br J Pharmacol 171 3485 PMID: 24758718

Pan et al (2011) Alterations of endocannabinoid signaling, synaptic plasticity, learning, and memory in monoacylglycerol lipase knock-out mice. J Cell Biol 31 13420 PMID: 21940435

Xiao et al (2018) OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons. Elife 7 PMID: 29676731

Johnston et al (2018) Activity in nodose ganglia neurons after treatment with CP 55,940 and cholecystokinin. Physiol Rep 6 e13927 PMID: 30512249

Hassanzadeh and Rostami (2014) CB1 cannabinoid receptors are involved in neuroleptic-induced enhancement of brain neurotensin. J Neurosci 17 181 PMID: 24847420

Gonzalez-Islas et al (2012) Tonic and transient endocannabinoid regulation of AMPAergic miniature postsynaptic currents and homeostatic plasticity in embryonic motor networks. Sci Rep 32 13597 PMID: 23015449

Chanda et al (2012) 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. Br J Pharmacol 287 38041 PMID: 22989885

Casarotto et al (2012) 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. Pain 37 478 PMID: 21937980

Niu et al (2012) Effects of gonadal hormones on the peripheral cannabinoid receptor 1 (CB1R) system under a myositis condition in rats. J Pharmacol Exp Ther 153 2283 PMID: 22940464

Bender et al (2006) Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex. J Neurosci 26 4166 PMID: 16624937

Cenni et al (2006) Differential effect of cannabinoid agonists and endocannabinoids on histamine release from distinct regions of the rat brain. Eur J Neurosci 24 1633 PMID: 17004927

Wang et al (2006) DArgic control of corticostriatal long-term synaptic depression in medium spiny neurons is mediated by cholinergic interneurons. Neuron 50 443 PMID: 16675398

Lin et al (2006) Effects of intra-amygdala infusion of CB1 receptor agonists on the reconsolidation of fear-potentiated startle. Learn Mem 13 316 PMID: 16705137

Laviolette (2006) Cannabinoids Potentiate Emotional Learning Plasticity in Neurons of the Medial Prefrontal Cortex through Basolateral Amygdala Inputs. J Neurosci 26 6458 PMID: 16775133

Nieri et al (2006) Modulation of P-glycoprotein activity by cannabinoid molecules in HK-2 renal cells. Br J Pharmacol 148 682 PMID: 16715117

Kettunen et al (2005) Neuromodulation via conditional release of endocannabinoids in the spinal locomotor network. Neuron 45 95 PMID: 15629705

Haj-Dahmane (2005) The wake-promoting peptide orexin-B inhibits glutamatergic transmission to dorsal raphe nucleus serotonin neurons through retrograde endocannabinoid signaling. J Neurosci 25 896 PMID: 15673670

de Oliveira Alvares et al (2005) Amnestic effect of intrahippocampal AM251, a CB1-selective blocker, in the inhibitory avoidance, but not in the open field habituation task, in rats. Neurobiol Learn Mem 83 119 PMID: 15721795

Safo and Regehr (2005) Endocannabinoids control the induction of cerebellar LTD. Neuron 48 647 PMID: 16301180

Malek et al (2015) Anandamide, Acting via CB2 Receptors, Alleviates LPS-Induced Neuroinflammation in Rat Primary Microglial Cultures. Neural Plast 2015 130639 PMID: 26090232

Zhang et al (2015) Anoctamin Calcium-Activated Chloride Channels May Modulate Inhibitory Transmission in the Cerebellar Cortex. PLoS One 10 e0142160 PMID: 26558388

Keimpema et al (2013) Diacylglycerol lipase α manipulation reveals developmental roles for intercellular endocannabinoid signaling. Nat Commun 3 2093 PMID: 23806960

Brents et al (2011) Phase I hydroxylated metabolites of the K2 synthetic cannabinoid JWH-018 retain in vitro and in vivo cannabinoid 1 receptor affinity and activity. PLoS One 6 e21917 PMID: 21755008

Crespillo et al (2011) Expression of the cannabinoid system in muscle: effects of a high-fat diet and CB1 receptor blockade. Biochem J 433 175 PMID: 20955176

Li and Burrell (2011) Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms. Learn Mem 18 545 PMID: 21844187

Ellermann et al (2020) Endocannabinoids inhibit the induction of virulence in enteric pathogens. Cell PMID: 33031742

Leroy et al (2017) Input-Timing-Dependent Plasticity in the Hippocampal CA2 Region and Its Potential Role in Social Memory. Neuron 95 1089 PMID: 28823730

Garzón et al (2009) Gz mediates the long-lasting desensitization of brain CB1 receptors and is essential for cross-tolerance with mor. Mol Pain 5 11 PMID: 19284549

Tjen-A-Looi et al (2009) Processing cardiovascular information in the vlPAG during electroacupuncture in rats: roles of endocannabinoids and GABA. J Appl Physiol (1985) 106 1793 PMID: 19325030

Mendiguren and Pineda (2009) Effect of the CB(1) receptor antagonists rim. and AM251 on the firing rate of dorsal raphe nucleus neurons in rat brain slices. Br J Pharmacol 158 1579 PMID: 19845674

Fraga et al (2009) Endogenous cannabinoids induce fever through the activation of CB1 receptors. Neuropsychopharmacology 157 1494 PMID: 19681872

Meuth et al (2009) The neuroprotective impact of the leak potassium channel TASK1 on stroke development in mice. Exp Neurol 33 42675 PMID: 18930826

Wallace et al (2009) PKCε regulates behavioral sensitivity, binding and tolerance to the CB1 receptor agonist WIN55,212-2. Iran J Basic Med Sci 34 1733 PMID: 19158669

Alharris et al (2019) Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget 10 45 PMID: 30713602

Diniz et al (2019) Dual mechanism of TRKB activation by anandamide through CB1 and TRPV1 receptors. PeerJ 7 e6493 PMID: 30809460

Saliba (2017) AM404, paracetamol metabolite, prevents prostaglandin synthesis in activated microglia by inhibiting COX activity. J Neuroinflammation 14 246 PMID: 29237478

Zhang (2017) Orphan nuclear receptor ERRγ is a key regulator of human fibrinogen gene expression. PLoS One 12 e0182141 PMID: 28750085

Fatahi (2017) Involvement of cannabinoid system in the nucleus accumbens on delay-based decision making in the rat. Behav Brain Res. 337 107 PMID: 28987618

Tortoriello et al (2014) Miswiring the brain: △9-tetrahydrocannabinol disrupts cortical development by inducing an SCG10/stathmin-2 degradation pathway. Proc Natl Acad Sci U S A 33 668 PMID: 24469251

Szabó et al (2014) Presynaptic calcium channel inhibition underlies CB1 cannabinoid receptor-mediated suppression of GABA release. Mediators Inflamm 34 7958 PMID: 24899717

Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. J Neurosci 5 4421 PMID: 25030704

Sreevalsan and Safe (2013) The cannabinoid WIN 55,212-2 decreases specificity protein transcription factors and the oncogenic cap protein eIF4E in colon cancer cells. Mol Cancer Ther 12 2483 PMID: 24030632

Wargent et al (2013) The cannabinoid δ(9)-tetrahydrocannabivarin (THCV) ameliorates Ins sensitivity in two mouse models of obesity. Nutr Diabetes 3 e68 PMID: 23712280

Chanda et al (2013) Hepatic cannabinoid receptor type 1 mediates alcohol-induced regulation of bile acid enzyme genes expression via CREBH. PLoS One 8 e68845 PMID: 23894352

Benz et al (2013) Expression and functional relevance of cannabinoid receptor 1 in Hodgkin lymphoma. PLoS One 8 e81675 PMID: 24349109

Malenczyk et al (2013) CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release. J Biol Chem 288 32685 PMID: 24089517

Abush and Akirav (2013) Cannabinoids ameliorate impairments induced by chronic stress to synaptic plasticity and short-term memory. Neuropsychopharmacology 38 1521 PMID: 23426383

Cao et al (2013) Cannabinoid HU210 protects isolated rat stomach against impairment caused by serum of rats with experimental acute pancreatitis. PLoS One 7 e52921 PMID: 23285225

Thompson and Perkel (2011) Endocannabinoids mediate synaptic plasticity at glutamatergic synapses on spiny neurons within a basal ganglia nucleus necessary for song learning. J Neurophysiol 105 1159 PMID: 21177997

Sousa et al (2011) 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. Neuropsychopharmacology 36 472 PMID: 20927050

Samineni et al (2011) Post-ictal analgesia in genetically epilepsy-prone rats is induced by audiogenic seizures and involves cannabinoid receptors in the periaqueductal gray. Brain Res 1389 177 PMID: 21439272

Segev and Akirav (2011) Differential effects of cannabinoid receptor agonist on social discrimination and contextual fear in amygdala and hippocampus. Learn Mem 18 254 PMID: 21447623

Guidali et al (2011) Cannabinoid CB1 receptor antagonism prevents neurochemical and behavioural deficits induced by chronic phencyclidine. Int J Neuropsychopharmacol 14 17 PMID: 20196921

Negrete et al (2011) The antinociceptive effects of JWH-015 in chronic inflammatory pain are produced by nitric oxide-cGMP-PKG-KATP pathway activation mediated by opioids. PLoS One 6 e26688 PMID: 22031841

Novellis et al (2011) 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. Mol Pain 7 7 PMID: 21241462

Ruby et al (2011) Acute overactive endocannabinoid signaling induces glucose intolerance, hepatic steatosis, and novel cannabinoid receptor 1 responsive genes. PLoS One 6 e26415 PMID: 22073164

Hassanzadeh and Hassanzadeh (2011) The Role of the Endocannabinoids in Suppression of the Hypothalamic-pituitary-adrenal Axis Activity by dox. J Leukoc Biol 14 414 PMID: 23493814

Pan et al (2009) 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. J Pharmacol Exp Ther 331 591 PMID: 19666749

Pacheco et al (2009) Central antinociception induced by mu-opioid receptor agonist morphine, but not delta- or kappa-, is mediated by cannabinoid CB1 receptor. Br J Pharmacol 158 225 PMID: 19594755

Ho and Gardiner (2009) Acute hypertension reveals depressor and vasodilator effects of cannabinoids in conscious rats. Br J Pharmacol 156 94 PMID: 19133994

Han (2017) Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation. Brain Res 1663 132 PMID: 28322749

King-Himmelreich (2017) AMPK contributes to aerobic exercise-induced antinociception downstream of endocannabinoids. Neuropharmacology 124 134 PMID: 28479394

Ma et al (2015) Mitochondrial CB1 receptor is involved in ACEA-induced protective effects on neurons and mitochondrial functions. Sci Rep 5 12440 PMID: 26215450

Stornaiuolo et al (2015) Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments. Sci Rep 5 15453 PMID: 26482099

Arrabal et al (2015) Pharmacological Blockade of Cannabinoid CB1 Receptors in Diet-Induced Obesity Regulates Mitochondrial Dihydrolipoamide Dehydrogenase in Muscle. PLoS One 10 e0145244 PMID: 26671069

Wang et al (2015) Activation of cannabinoid receptor 1 inhibits increased bladder activity induced by nerve growth factor. Neurosci Lett 589 19 PMID: 25575795

Bashashati et al (2015) Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation. Br J Pharmacol 172 3099 PMID: 25684407

Parvathy and Masocha (2015) Coadministration of indomet. and MinCyc attenuates established PacT.-induced neuropathic thermal hyperalgesia: Involvement of cannabinoid CB1 receptors. J Neurosci 5 10541 PMID: 26085115

Krishnan and Chatterjee (2015) Differential immune mechanism to HIV-1 Tat variants and its regulation by AEA [corrected]. PLoS One 5 9887 PMID: 25943894

Merighi et al (2012) Cannabinoid CB(2) receptor attenuates morphine-induced inflammatory responses in activated microglial cells. Br J Pharmacol 166 2371 PMID: 22428664

Méndez-Díaz et al (2012) The endocannabinoid system modulates the valence of the emotion associated to food ingestion. Addict Biol 17 725 PMID: 21182571

Hamtiaux et al (2012) The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action. BMC Cancer 12 92 PMID: 22429826

Aydin et al (2012) 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. Neuropharmacology 63 1335 PMID: 22959963

Baur et al (2012) The cannabinoid CB1 receptor antagonists rim. (SR141716) and AM251 directly potentiate GABA(A) receptors. Br J Pharmacol 165 2479 PMID: 21470203

Hamtiaux et al (2011) Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism. PLoS One 6 e26823 PMID: 22046372

Touriño et al (2010) THC Prevents MDMA Neurotoxicity in Mice. PLoS One 5 e9143 PMID: 20174577

Losonczy et al (2010) Network mechanisms of theta related neuronal activity in hippocampal CA1 pyramidal neurons. Nat Neurosci 13 967 PMID: 20639875

Wamsteeker et al (2010) Repeated stress impairs endocannabinoid signaling in the paraventricular nucleus of the hypothalamus. J Neurosci 30 11188 PMID: 20720126

Huang et al (2010) A refractory period for rejuvenating GABAergic synaptic transmission and ocular dominance plasticity with dark exposure. J Neurosci 30 16636 PMID: 21148002

Hoffman et al (2010) Control of cannabinoid CB1 receptor function on glutamate axon terminals by endogenous adenosine acting at A1 receptors. J Neurosci 30 545 PMID: 20071517

Godlewski et al (2010) Inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in hypertension without adverse metabolic effects. Chem Biol 17 1256 PMID: 21095576

Zhang et al (2010) Cannabinoid CB1 receptor facilitation of substance P release in the rat spinal cord, measured as neurokinin 1 receptor internalization. Eur J Neurosci 31 225 PMID: 20074214

Bhaskaran and Smith (2010) Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy. Endocrinology 223 529 PMID: 20144892

Sinnayah et al Feeding induced by cannabinoids is mediated independently of the melanocortin system. Proc Natl Acad Sci U S A 3 e2202 PMID: 18493584

Kola et al The orexigenic effect of ghrelin is mediated through central activation of the endogenous cannabinoid system. Br J Pharmacol 3 e1797 PMID: 18335063

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Jiang et al Expression and function of cannabinoid receptors CB1 and CB2 and their cognate cannabinoid ligands in murine embryonic stem cells. PLoS One 2 e641 PMID: 17653268

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CB1R antagonist AM251 (5 µM).
By Kang Peng on 09/18/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: auditory brainstem(MNTB)

bath application of the CB1R antagonist AM251 (5 µM)

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