Nanomolar affinity cannabinoid receptor agonist (K
values are 62.3 and 3.3 nM at the human cloned CB
receptors respectively). S-enantiomer
WIN 55,212-3 mesylate
(Cat. No. 2327) also available.
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The citations listed below are publications that use Tocris products. Selected citations for WIN 55,212-2 mesylate include:
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Feeding induced by cannabinoids is mediated independently of the melanocortin system. Authors: Sinnayah Et al. Endocrinology ;3:e2202 Cannabinoids reduce markers of inflammation and fibrosis in pancreatic stellate cells. Authors: Michalski Et al. Am J Physiol Gastrointest Liver Physiol ;3:e1701 The synthetic cannabinoid WIN-55,212-55,212 induced-apoptosis in cytotrophoblasts cells by a mechanism dependent on CB1 receptor. Authors: Almada Toxicology 2017;385:67 Characterization of structurally novel G protein biased CB1 agonists: implications for drug development. Authors: Ford Pharmacol Res 2017;125:161 Decreased CB receptor binding and cannabinoid signaling in three brain regions of a rat model of schizophrenia Authors: Szücs Et al. Neuroscience Letters 2016;633:87 WIN 55,212-2 inhibits the epithelial mesenchymal transition of gastric cancer cells via COX-2 signals Authors: Xian Et al. Cell Physiology and Biochemistry 2016;39:2149 Somatostatin receptor 5 is a prominent regulator of signaling pathways in cells with coexpression of Cannabinoid receptors 1 Authors: Zou Et al. Neuroscience 2016;340:218 Correlations between the Memory-Related Behavior and the Level of Oxidative Stress Biomarkers in the Mice Brain, Provoked by an Acute Administration of CB Receptor Ligands. Authors: Kruk-Slomka Et al. Neural Plast 2016;2016:9815092 Cannabinoid WIN-55,212-2 mesylate inhibits ADAMTS-4 activity in human osteoarthritic articular chondrocytes by inhibiting expression of syndecan-1. Authors: Kong Et al. Int J Neuropsychopharmacol 2016;13:4569 (4-(Bis(4-fluorophenyl)methyl)piperazin-1-yl)(cyclohexyl)methanone hydrochloride (LDK1229): a new cannabinoid CB1 receptor inverse agonist from the class of benzhydryl piperazine analogs. Authors: Mahmoud Et al. Mol Pharmacol 2015;87:197 TRPA1 mediates the hypothermic action of acetaminophen. Authors: Gentry Et al. Br J Pharmacol 2015;5:12771 Behavioral and neurochemical changes in mesostriatal dopaminergic regions of the rat after chronic administration of the cannabinoid receptor agonist WIN55,212-2. Authors: Fanarioti Et al. Int J Mol Sci 2015;18 Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. Authors: Lin Et al. Sci Rep 2015;16:5555 The cannabinoid agonist HU-210: pseudo-irreversible discriminative stimulus effects in rhesus monkeys. Authors: Hruba and McMahon Neuropharmacology 2014;727:35 Ligand-specific endocytic dwell times control functional selectivity of the cannabinoid receptor 1. Authors: Flores-Otero Et al. Nat Commun 2014;5:4589 Effects of cannabinoid drugs on the deficit of prepulse inhibition of startle in an animal model of schizophrenia: the SHR strain. Authors: Levin Et al. Eur J Pharmacol 2014;5:10 Miswiring the brain: △9-tetrahydrocannabinol disrupts cortical development by inducing an SCG10/stathmin-2 degradation pathway. Authors: Tortoriello Et al. Br J Pharmacol 2014;33:668 The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. Authors: Sánchez-Blázquez Et al. Mol Med Rep 2014;17:1943 Inhibition of p38/Mk2 signaling pathway improves the anti-inflammatory effect of WIN55 on mouse experimental colitis. Authors: Li Et al. Lab Invest 2013;93:322 CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity. Authors: Baillie Et al. Mol Pharmacol 2013;83:322 Fluoxetine impairs GABAergic signaling in hippocampal slices from neonatal rats. Authors: Caiati and Cherubini Front Cell Neurosci 2013;7:63 CB1 and CB2 receptors are novel molecular targets for Tamoxifen and 4OH-Tamoxifen. Authors: Prather Et al. Biochem Biophys Res Commun 2013;441:339 Cannabinoids ameliorate impairments induced by chronic stress to synaptic plasticity and short-term memory. Authors: Abush and Akirav Neuropsychopharmacology 2013;38:1521 Novel insights into CB1 cannabinoid receptor signaling: a key interaction identified between the extracellular-3 loop and transmembrane helix 2. Authors: Marcu Et al. J Pharmacol Exp Ther 2013;345:189 Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Authors: Marini Et al. Br J Pharmacol 2013;169:887 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 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 CB1 receptor autoradiographic characterization of the individual differences in approach and avoidance motivation. Authors: Laricchiuta Et al. PLoS One 2012;7:e42111 Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Authors: Caiati Et al. Sci Rep 2012;2:285 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 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 Cannabinoids attenuate hippocampal γ oscillations by suppressing excitatory synaptic input onto CA3 pyramidal neurons and fast spiking basket cells. Authors: Holderith Et al. J Neurosci 2011;589:4921 Cannabinoid receptors, CB1 and CB2, as novel targets for inhibition of non-small cell lung cancer growth and metastasis. Authors: Preet Et al. Cancer Prev Res (Phila) 2011;4:65 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 The atypical cannabinoid O-1602 protects against experimental colitis and inhibits neutrophil recruitment. Authors: Schicho Et al. Inflamm Bowel Dis 2011;17:1651 The cannabinoid WIN55,212-2 protects against oxidized LDL-induced inflammatory response in murine macrophages. Authors: Hao Et al. J Neurosci 2010;51:2181 Cannabidiol displays antiepileptiform and antiseizure properties in vitro and in vivo. Authors: Jones Et al. Br J Pharmacol 2010;332:569 Selective reduction of cholecystokinin-positive basket cell innervation in a model of temporal lobe epilepsy. Authors: Wyeth Et al. J Neurosci 2010;30:8993 Cannabinoids excite circadian clock neurons. Authors: Acuna-Goycolea Et al. PLoS One 2010;30:10061 Retrograde endocannabinoid signaling reduces GABAergic synaptic transmission to gonadotropin-releasing hormone neurons. Authors: Farkas Et al. J Biomol Screen 2010;151:5818 Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses. Authors: Kim and Alger Nat Neurosci 2010;13:592 Gz mediates the long-lasting desensitization of brain CB1 receptors and is essential for cross-tolerance with morphine. Authors: Garzón Et al. Mol Pain 2009;5:11 Cannabinoid regulation of nitric oxide synthase I (nNOS) in neuronal cells. Authors: Carney Et al. J Neuroimmune Pharmacol 2009;4:338 Effects of cannabinoids on caffeine contractures in slow and fast skeletal muscle fibers of the frog. Authors: Huerta Et al. J Membr Biol 2009;229:91 Acute hypertension reveals depressor and vasodilator effects of cannabinoids in conscious rats. Authors: Ho and Gardiner Front Pharmacol 2009;156:94 Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter β-arrestin assay. Authors: McGuinness Et al. Int J Neuropsychopharmacol 2009;14:49 TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons. Authors: Gibson Et al. Neuron 2008;57:746 Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others. Authors: Karson Et al. J Physiol 2008;54:117 Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction. Authors: Kapur Et al. J Pharmacol Exp Ther 2008;325:341 The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms. Authors: Potenzieri Et al. Brain Res 2008;1215:69 N-arachidonoyl-dopamine tunes synaptic transmission onto dopaminergic neurons by activating both cannabinoid and vanilloid receptors. Authors: Marinelli Et al. Neuropsychopharmacology 2007;32:298 Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons. Authors: Kelm Et al. J Neurosci 2007;323:356 Tonic enhancement of endocannabinoid-mediated retrograde suppression of inhibition by cholinergic interneuron activity in the striatum. Authors: Narushima Et al. J Neurosci 2007;27:496 Cannabinoids excite hypothalamic melanin-concentrating hormone but inhibit hypocretin/orexin neurons: implications for cannabinoid actions on food intake and cognitive arousal. Authors: Huang Et al. J Neurosci 2007;27:4870 The psychoactive plant cannabinoid, Delta9-tetrahydrocannabinol, is antagonized by Delta8- and Delta9-tetrahydrocannabivarin in mice in vivo. Authors: Pertwee Et al. Br J Pharmacol 2007;150:586 Species and strain differences in the expression of a novel glutamate-modulating cannabinoid receptor in the rodent hippocampus. Authors: Hoffman Et al. J Lipid Res 2005;22:2387 Evidence that the plant cannabinoid Delta9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist. Authors: Thomas Et al. Br J Pharmacol 2005;146:917 Distribution and function of the cannabinoid-1 receptor in the modulation of ion transport in the guinea pig ileum: relationship to capsaicin-sensitive nerves. Authors: MacNaughton Et al. Eur J Neurosci 2004;286:G863 Electrical coupling among irregular-spiking GABAergic interneurons expressing cannabinoid receptors. Authors: Galarreta Et al. J Pharmacol Exp Ther 2004;24:9770 Repeated treatment with the synthetic cannabinoid WIN 55,212-2 reduces both hyperalgesia and production of pronociceptive mediators in a rat model of neuropathic pain. Authors: Costa Et al. J Neurosci 2004;141:42586 The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response. Authors: Williams Et al. EMBO J 2003;160:481 A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus. Authors: Craib Et al. PLoS One 2001;134:42581
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