Key Product Details
Description: | Selective high affinity CB2 agonist |
Alternative Names: | (R)-(+)-WIN 55212 |
Chemical Name: | (R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone mesylate |
Purity: | ≥98% (HPLC) |
Molecular Weight: | 522.61 |
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Citations for WIN 55,212-2 mesylate (113)
Citations are publications that use Bio-Techne products. Selected citations for WIN 55,212-2 mesylate include:
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Pedersen et al.
(2021)
A novel luminescence-based-β-arrestin recruitment assay for unmodified receptors
J Biol Chem.
296:100503
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Diniz et al.
(2019)
Dual mechanism of TRKB activation by anandamide through CB1 and TRPV1 receptors.
PeerJ.
7:e6493
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Xiao et al.
(2018)
OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons.
Elife.
7
PMID: 29676731 -
Tan and Cao
(2018)
Cannabinoid WIN-55,212-2 mesylate inhibits tumor necrosis factor-α-induced expression of nitric oxide synthase in dorsal root ganglion neurons.
Int J Mol Med.
42:919
PMID: 29786105 -
Hegyi et al.
(2018)
CB1 receptor activation induces intracellular Ca2+ mobilization and 2-arachidonoylglycerol release in rodent spinal cord astrocytes.
Sci Rep.
8:10562
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Balleza-Tapia et al.
(2018)
TrpV1 receptor activation rescues neuronal function and network gamma oscillations from Aβ-induced impairment in mouse hippocampus in vitro.
Elife.
7
PMID: 30417826 -
Mouro et al.
(2018)
Chronic, intermittent treatment with a cannabinoid receptor agonist impairs recognition memory and brain network functional connectivity.
J Neurochem.
147:71
PMID: 29989183 -
Khan et al.
(2018)
Involvement of the CB2 cannabinoid receptor in cell growth inhibition and G0/G1 cell cycle arrest via the cannabinoid agonist WIN 55,212-2 in renal cell carcinoma.
BMC Cancer.
18:583
PMID: 29792186 -
Almada
(2017)
The synthetic cannabinoid WIN-55,212-55,212 induced-apoptosis in cytotrophoblasts cells by a mechanism dependent on CB1 receptor.
Toxicology.
385:67
PMID: 28495606 -
Ford
(2017)
Characterization of structurally novel G protein biased CB1 agonists: implications for drug development.
Pharmacol Res.
125:161
PMID: 28838808 -
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 -
Baker et al.
(2017)
Big conductance calcium-activated potassium channel openers control spasticity without sedation.
Br J Pharmacol.
174:2662
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Hashimotodani et al.
(2017)
LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance.
Neuron.
95:928
PMID: 28817805 -
Kruk-Slomka et al.
(2016)
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.
Neural Plast.
2016:9815092
PMID: 26839719 -
Kong et al.
(2016)
Cannabinoid WIN-55,212-2 mesylate inhibits ADAMTS-4 activity in human osteoarthritic articular chondrocytes by inhibiting expression of syndecan-1.
Int J Neuropsychopharmacol.
13:4569
PMID: 27082728 -
Szücs et al.
(2016)
Decreased CB receptor binding and cannabinoid signaling in three brain regions of a rat model of schizophrenia
Neuroscience Letters.
633:87
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Zou et al.
(2016)
Somatostatin receptor 5 is a prominent regulator of signaling pathways in cells with coexpression of Cannabinoid receptors 1
Neuroscience.
340:218
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Xian et al.
(2016)
WIN 55,212-2 inhibits the epithelial mesenchymal transition of gastric cancer cells via COX-2 signals
Cell Physiology and Biochemistry.
39:2149
PMID: 27802436 -
Pinheiro et al.
(2016)
Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin.
Brain Res Bull.
124:222
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Seo et al.
(2016)
Regulation of divalent metal transporter-1 by serine phosphorylation.
Biochem J.
473:4243
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Yu et al.
(2016)
Dentate cannabinoid-sensitive interneurons undergo unique and selective strengthening of mutual synaptic inhibition in experimental epilepsy.
Neurobiol Dis.
89:23
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Mahmoud et al.
(2015)
(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.
Mol Pharmacol.
87:197
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Fanarioti et al.
(2015)
Behavioral and neurochemical changes in mesostriatal DArgic regions of the rat after chronic administration of the cannabinoid receptor agonist WIN55,212-2.
Int J Mol Sci.
18
PMID: 25522428 -
Lin et al.
(2015)
Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
Sci Rep.
16:5555
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Gentry et al.
(2015)
TRPA1 mediates the hypothermic action of acetaminophen.
Br J Pharmacol.
5:12771
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Flores-Otero et al.
(2014)
Ligand-specific endocytic dwell times control functional selectivity of the cannabinoid receptor 1.
Nat Commun.
5:4589
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Sánchez-Blázquez et al.
(2014)
The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases.
Mol Med Rep.
17:1943
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Levin et al.
(2014)
Effects of cannabinoid drugs on the deficit of prepulse inhibition of startle in an animal model of schizophrenia: the SHR strain.
Eur J Pharmacol.
5:10
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Tortoriello et al.
(2014)
Miswiring the brain: △9-tetrahydrocannabinol disrupts cortical development by inducing an SCG10/stathmin-2 degradation pathway.
Br J Pharmacol.
33:668
PMID: 24469251 -
Hruba and McMahon
(2014)
The cannabinoid agonist HU-210: pseudo-irreversible discriminative stimulus effects in rhesus monkeys.
Neuropharmacology.
727:35
PMID: 24486701 -
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 -
Li et al.
(2013)
Inhibition of p38/Mk2 signaling pathway improves the anti-inflammatory effect of WIN55 on mouse experimental colitis.
Lab Invest.
93:322
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Marini et al.
(2013)
Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors.
Br J Pharmacol.
169:887
PMID: 23711022 -
Abush and Akirav
(2013)
Cannabinoids ameliorate impairments induced by chronic stress to synaptic plasticity and short-term memory.
Neuropsychopharmacology.
38:1521
PMID: 23426383 -
Baillie et al.
(2013)
CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity.
Mol Pharmacol.
83:322
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Caiati and Cherubini
(2013)
Fluoxetine impairs GABAergic signaling in hippocampal slices from neonatal rats.
Front Cell Neurosci.
7:63
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Marcu et al.
(2013)
Novel insights into CB1 cannabinoid receptor signaling: a key interaction identified between the extracellular-3 loop and transmembrane helix 2.
J Pharmacol Exp Ther.
345:189
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Prather et al.
(2013)
CB1 and CB2 receptors are novel molecular targets for tamox. and 4OH-Tamoxifen.
Biochem Biophys Res Commun.
441:339
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Cawston et al.
(2013)
Real-time characterization of cannabinoid receptor 1 (CB1 ) allosteric modulators reveals novel mechanism of action.
Br J Pharmacol.
170:893
PMID: 23937487 -
Uhelski et al.
(2013)
The non-selective cannabinoid receptor agonist WIN 55,212-2 attenuates responses of C-fiber nociceptors in a murine model of cancer pain.
Neuroscience.
247:84
PMID: 23673278 -
Kargl et al.
(2013)
A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function.
J Pharmacol Exp Ther.
346:54
PMID: 23639801 -
Akerman et al.
(2013)
Endocannabinoids in the brainstem modulate dural trigeminovascular nociceptive traffic via CB1 and "triptan" receptors: implications in migraine.
J Neurosci.
33:14869
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Caiati et al.
(2012)
Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
Sci Rep.
2:285
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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 -
Segev et al.
(2012)
Stress hormones receptors in the amygdala mediate the effects of stress on the consolidation, but not the retrieval, of a non aversive spatial task.
PLoS One.
7:e29988
PMID: 22253850 -
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 -
Zhong et al.
(2012)
Phosphodiesterase 4 inhibition impairs cocaine-induced inhibitory synaptic plasticity and conditioned place preference.
Neuropsychopharmacology.
37:2377
PMID: 22713909 -
Kargl et al.
(2012)
The cannabinoid receptor CB1 modulates the signaling properties of the lysophosphatidylinositol receptor GPR55.
J Biol Chem.
287:44234
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Kazemi et al.
(2012)
Effect of cannabinoid receptor activation on spreading depression.
Iran J Basic Med Sci.
15:926
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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 -
Abush and Akirav
(2012)
Short- and long-term cognitive effects of chronic cannabinoids administration in late-adolescence rats.
PLoS One.
7:e31731
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Izzo et al.
(2012)
Inhibitory effect of cannabichromene, a major non-psychotropic cannabinoid extracted from Cannabis sativa, on inflammation-induced hypermotility in mice.
Br J Pharmacol.
166:1444
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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
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Schicho et al.
(2011)
The atypical cannabinoid O-1602 protects against experimental colitis and inhibits neutrophil recruitment.
Inflamm Bowel Dis.
17:1651
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Preet et al.
(2011)
Cannabinoid receptors, CB1 and CB2, as novel targets for inhibition of non-small cell lung cancer growth and metastasis.
Cancer Prev Res (Phila).
4:65
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Holderith et al.
(2011)
Cannabinoids attenuate hippocampal γ oscillations by suppressing excitatory synaptic input onto CA3 pyramidal neurons and fast spiking basket cells.
J Neurosci.
589:4921
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Pan et al.
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Alterations of endocannabinoid signaling, synaptic plasticity, learning, and memory in monoacylglycerol lipase knock-out mice.
J Cell Biol.
31:13420
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Tozzi et al.
(2011)
The distinct role of medium spiny neurons and cholinergic interneurons in the D2/A2A receptor interaction in the striatum: implications for Parkinson's disease.
J Neurosci.
31:1850
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Tan et al.
(2011)
Cannabinoid transmission in the basolateral amygdala modulates fear memory formation via functional inputs to the prelimbic cortex.
J Neurosci.
31:5300
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Okada et al.
(2011)
High extracellular Ca2+ stimulates Ca2+-activated Cl- currents in frog parathyroid cells through the mediation of arachidonic acid cascade.
PLoS One.
6:e19158
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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
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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
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Lecca et al.
(2011)
Effects of drugs of abuse on putative rostromedial tegmental neurons, inhibitory afferents to midbrain DA cells.
Neuropsychopharmacology.
36:589
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Wyeth et al.
(2010)
Selective reduction of cholecystokinin-positive basket cell innervation in a model of temporal lobe epilepsy.
J Neurosci.
30:8993
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Kim and Alger
(2010)
Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses.
Nat Neurosci.
13:592
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Acuna-Goycolea et al.
(2010)
Cannabinoids excite circadian clock neurons.
PLoS One.
30:10061
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Farkas et al.
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Retrograde endocannabinoid signaling reduces GABAergic synaptic transmission to gonadotropin-releasing hormone neurons.
J Biomol Screen.
151:5818
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Jones et al.
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Cannabidiol displays antiepileptiform and antiseizure properties in vitro and in vivo.
Br J Pharmacol.
332:569
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Hao et al.
(2010)
The cannabinoid WIN55,212-2 protects against oxidized LDL-induced inflammatory response in murine macrophages.
J Neurosci.
51:2181
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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
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Garzón et al.
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Gz mediates the long-lasting desensitization of brain CB1 receptors and is essential for cross-tolerance with mor.
Mol Pain.
5:11
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Huerta et al.
(2009)
Effects of cannabinoids on caffeine contractures in slow and fast skeletal muscle fibers of the frog.
J Membr Biol.
229:91
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Carney et al.
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Cannabinoid regulation of nitric oxide synthase I (nNOS) in neuronal cells.
J Neuroimmune Pharmacol.
4:338
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McGuinness et al.
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Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter β-arrestin assay.
Int J Neuropsychopharmacol.
14:49
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Ho and Gardiner
(2009)
Acute hypertension reveals depressor and vasodilator effects of cannabinoids in conscious rats.
Front Pharmacol.
156:94
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Price et al.
(2009)
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.
Eur J Neurosci.
29:2177
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Gibson et al.
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TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons.
Neuron.
57:746
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Kapur et al.
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Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction.
J Pharmacol Exp Ther.
325:341
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Potenzieri et al.
(2008)
The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms.
Brain Res.
1215:69
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Karson et al.
(2008)
Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others.
J Physiol.
54:117
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Chiu and Castillo
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Input-specific plasticity at excitatory synapses mediated by endocannabinoids in the dentate gyrus.
Neuropharmacology.
54:68
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Huang et al.
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Roles of endocannabinoids in heterosynaptic long-term depression of excitatory synaptic transmission in visual cortex of young mice.
J Neurosci.
28:7074
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Kelm et al.
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The role of protein kinase A in the ethanol-induced increase in spontaneous GABA release onto cerebellar Purkinje neurons.
J Neurophysiol.
100:3417
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Kim et al.
(2008)
Interactions between CB(1) receptors and TRPV1 channels mediated by 12-HPETE are cytotoxic to mesencephalic DArgic neurons.
Br J Pharmacol.
155:253
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Huang et al.
(2007)
Cannabinoids excite hypothalamic melanin-concentrating hormone but inhibit hypocretin/orexin neurons: implications for cannabinoid actions on food intake and cognitive arousal.
J Neurosci.
27:4870
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Pertwee et al.
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The psychoactive plant cannabinoid, Delta9-tetrahydrocannabinol, is antagonized by Delta8- and Delta9-tetrahydrocannabivarin in mice in vivo.
Br J Pharmacol.
150:586
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Marinelli et al.
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N-arachidonoyl-DA tunes synaptic transmission onto DArgic neurons by activating both cannabinoid and vanilloid receptors.
Neuropsychopharmacology.
32:298
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Kelm et al.
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Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons.
J Neurosci.
323:356
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Narushima et al.
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Tonic enhancement of endocannabinoid-mediated retrograde suppression of inhibition by cholinergic interneuron activity in the striatum.
J Neurosci.
27:496
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Cachope et al.
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Potentiation of electrical and chemical synaptic transmission mediated by endocannabinoids.
Neuron.
56:1034
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Hoffman et al.
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Opposing actions of chronic Delta9-tetrahydrocannabinol and cannabinoid antagonists on hippocampal long-term potentiation.
Learn Mem.
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Akerman et al.
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Cannabinoid (CB1) receptor activation inhibits trigeminovascular neurons.
J Pharmacol Exp Ther.
320:64
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Monory et al.
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The endocannabinoid system controls key epileptogenic circuits in the hippocampus.
Neuron.
51:455
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Thomas et al.
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Evidence that the plant cannabinoid Delta9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist.
Br J Pharmacol.
146:917
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Hoffman et al.
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Species and strain differences in the expression of a novel glutamate-modulating cannabinoid receptor in the rodent hippocampus.
J Lipid Res.
22:2387
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Okada et al.
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Biophysical properties of voltage-gated Na+ channels in frog parathyroid cells and their modulation by cannabinoids.
J Exp Biol.
208:4747
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Kettunen et al.
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Neuromodulation via conditional release of endocannabinoids in the spinal locomotor network.
Neuron.
45:95
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Haj-Dahmane
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The wake-promoting peptide orexin-B inhibits glutamatergic transmission to dorsal raphe nucleus serotonin neurons through retrograde endocannabinoid signaling.
J Neurosci.
25:896
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Costa et al.
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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.
J Neurosci.
141:42586
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Galarreta et al.
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Electrical coupling among irregular-spiking GABAergic interneurons expressing cannabinoid receptors.
J Pharmacol Exp Ther.
24:9770
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MacNaughton et al.
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Distribution and function of the cannabinoid-1 receptor in the modulation of ion transport in the guinea pig ileum: relationship to capsaicin-sensitive nerves.
Eur J Neurosci.
286:G863
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Melis et al.
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Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in DA neurons.
J Neurosci.
24:10707
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Williams et al.
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The FGF receptor uses the endocannabinoid signaling system to couple to an axonal growth response.
EMBO J.
160:481
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Barann et al.
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Direct inhibition by cannabinoids of human 5-HT3A receptors: probable involvement of an allosteric modulatory site.
Br J Pharmacol.
137:589
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McKallip et al.
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Targeting CB2 cannabinoid receptors as a novel therapy to treat malignant lymphoblastic disease.
Blood.
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Craib et al.
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A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus.
PLoS One.
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Bridges et al.
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The synthetic cannabinoid WIN55,212-2 attenuates hyperalgesia and allodynia in a rat model of neuropathic pain.
Br J Pharmacol.
133:586
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Izzo et al.
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Modulation of peristalsis by cannabinoid CB(1) ligands in the isolated guinea-pig ileum.
Br J Pharmacol.
129:984
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Izzo et al.
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Central and peripheral cannabinoid modulation of gastrointestinal transit in physiological states or during the diarrhoea induced by croton oil.
Br J Pharmacol.
129:1627
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Sinnayah et al.
Feeding induced by cannabinoids is mediated independently of the melanocortin system.
Endocrinology.
3:e2202
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Michalski et al.
Cannabinoids reduce markers of inflammation and fibrosis in pancreatic stellate cells.
Am J Physiol Gastrointest Liver Physiol.
3:e1701
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