Nanomolar affinity cannabinoid receptor agonist (K
values are 62.3 and 3.3 nM at the human cloned CB
S-enantiomer also available.
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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.
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.
Involvement of cannabinoid system in the nucleus accumbens on delay-based decision making in the rat.
Behav Brain Res. 2017;337:107
Characterization of structurally novel G protein biased CB1 agonists: implications for drug development.
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.
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
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
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
The non-selective cannabinoid receptor agonist WIN 55,212-2 attenuates responses of C-fiber nociceptors in a murine model of cancer pain.
Authors: Uhelski Et al.
Real-time characterization of cannabinoid receptor 1 (CB1 ) allosteric modulators reveals novel mechanism of action.
Authors: Cawston Et al.
Br J Pharmacol 2013;170:893
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
Short- and long-term cognitive effects of chronic cannabinoids administration in late-adolescence rats.
Authors: Abush and Akirav
PLoS One 2012;7:e31731
Stress hormones receptors in the amygdala mediate the effects of stress on the consolidation, but not the retrieval, of a non aversive spatial task.
Authors: Segev Et al.
PLoS One 2012;7:e29988
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
Phosphodiesterase 4 inhibition impairs cocaine-induced inhibitory synaptic plasticity and conditioned place preference.
Authors: Zhong Et al.
Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
Authors: Caiati Et al.
Sci Rep 2012;2:285
The cannabinoid receptor CB1 modulates the signaling properties of the lysophosphatidylinositol receptor GPR55.
Authors: Kargl Et al.
J Biol Chem 2012;287:44234
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
Effect of cannabinoid receptor activation on spreading depression.
Authors: Kazemi Et al.
Iran J Basic Med Sci 2012;15:926
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
High extracellular Ca2+ stimulates Ca2+-activated Cl- currents in frog parathyroid cells through the mediation of arachidonic acid cascade.
Authors: Okada Et al.
PLoS One 2011;6:e19158
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
Effects of drugs of abuse on putative rostromedial tegmental neurons, inhibitory afferents to midbrain dopamine cells.
Authors: Lecca Et al.
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.
Cannabinoid transmission in the basolateral amygdala modulates fear memory formation via functional inputs to the prelimbic cortex.
Authors: Tan Et al.
J Neurosci 2011;31:5300
The distinct role of medium spiny neurons and cholinergic interneurons in the D2/A2A receptor interaction in the striatum: implications for Parkinson's disease.
Authors: Tozzi Et al.
J Neurosci 2011;31:1850
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
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
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
WIN55,212-2, a cannabinoid receptor agonist, protects against nigrostriatal cell loss in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine mouse model of Parkinson's disease.
Authors: Price Et al.
Eur J Neurosci 2009;29:2177
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.
Input-specific plasticity at excitatory synapses mediated by endocannabinoids in the dentate gyrus.
Authors: Chiu and Castillo
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
Potentiation of electrical and chemical synaptic transmission mediated by endocannabinoids.
Authors: Cachope Et al.
N-arachidonoyl-dopamine tunes synaptic transmission onto dopaminergic neurons by activating both cannabinoid and vanilloid receptors.
Authors: Marinelli Et al.
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
Opposing actions of chronic Delta9-tetrahydrocannabinol and cannabinoid antagonists on hippocampal long-term potentiation.
Authors: Hoffman Et al.
Learn Mem 2007;14:63
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
Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in dopamine neurons.
Authors: Melis Et al.
J Neurosci 2004;24:10707
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
Direct inhibition by cannabinoids of human 5-HT3A receptors: probable involvement of an allosteric modulatory site.
Authors: Barann Et al.
Br J Pharmacol 2002;137:589
Targeting CB2 cannabinoid receptors as a novel therapy to treat malignant lymphoblastic disease.
Authors: McKallip Et al.
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
The synthetic cannabinoid WIN55,212-2 attenuates hyperalgesia and allodynia in a rat model of neuropathic pain.
Authors: Bridges Et al.
Br J Pharmacol 2001;133:586
Modulation of peristalsis by cannabinoid CB(1) ligands in the isolated guinea-pig ileum.
Authors: Izzo Et al.
Br J Pharmacol 2000;129:984
Central and peripheral cannabinoid modulation of gastrointestinal transit in physiological states or during the diarrhoea induced by croton oil.
Authors: Izzo Et al.
Br J Pharmacol 2000;129:1627
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