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Submit ReviewWIN 55,212-2 mesylate is a selective high affinity CB2 agonist (Ki values are 3.3 and 62.3 nM at the human cloned CB2 and CB1 receptors respectively).
分子量 | 522.61 |
公式 | C27H26N2O3.CH3SO3H |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 131543-23-2 |
PubChem ID | 6604176 |
InChI Key | FSGCSTPOPBJYSX-VEIFNGETSA-N |
Smiles | CS(O)(=O)=O.CC1=C(C(=O)C2=CC=CC3=C2C=CC=C3)C2=CC=CC3=C2N1[C@H](CN1CCOCC1)CO3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 15.68 | 30 温和加热 | |
DMSO | 52.26 | 100 温和加热 |
以下数据基于产品分子量 522.61。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.91 mL | 9.57 mL | 19.13 mL |
5 mM | 0.38 mL | 1.91 mL | 3.83 mL |
10 mM | 0.19 mL | 0.96 mL | 1.91 mL |
50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
参考文献是支持产品生物活性的出版物。
D'Ambra et al (1992) Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. J.Med.Chem. 35 124 PMID: 1732519
Felder et al (1995) Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors. Mol.Pharmacol. 48 443 PMID: 7565624
Griffin et al (1998) Evaluation of cannabinoid receptor agonists and antagonists using the guanosine-5'-O-(3-[35S]thio)-triphosphate binding assay in rat cerebellar membranes. J.Pharmacol.Exp.Ther. 285 553 PMID: 9580597
Martellotta et al (1998) Self-administration of the cannabinoid receptor agonist WIN 55,212-2 in drug naive mice. Neuroscience 85 327 PMID: 9622233
If you know of a relevant reference for WIN 55,212-2 mesylate, please let us know.
关键词: WIN 55,212-2 mesylate, WIN 55,212-2 mesylate supplier, potent, cannabinoid, agonists, Non-Selective, Cannabinoids, Receptors, WIN55212-2, mesylate, (R)-(+)-WIN55212, cb2r, cb1r, WIN552122, (R)-(+)-WIN, 55212, Non-selective, 1038, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 WIN 55,212-2 mesylate 的部分引用包括:
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Pedersen et al (2021) A novel luminescence-based-β-arrestin recruitment assay for unmodified receptors J Biol Chem 296 100503 PMID: 33684444
Diniz et al (2019) Dual mechanism of TRKB activation by anandamide through CB1 and TRPV1 receptors. PeerJ 7 e6493 PMID: 30809460
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
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 PMID: 24485144
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 PMID: 24567721
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
Caiati and Cherubini (2013) Fluoxetine impairs GABAergic signaling in hippocampal slices from neonatal rats. Front Cell Neurosci 7 63 PMID: 23641199
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 PMID: 23426954
Prather et al (2013) CB1 and CB2 receptors are novel molecular targets for tamox. and 4OH-Tamoxifen. Biochem Biophys Res Commun 441 339 PMID: 24148245
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 PMID: 23381627
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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 PMID: 21559478
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
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 PMID: 21471365
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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 PMID: 21048703
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 PMID: 19490092
Ho and Gardiner (2009) Acute hypertension reveals depressor and vasodilator effects of cannabinoids in conscious rats. Front Pharmacol 156 94 PMID: 19133994
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
Abush and Akirav (2012) Short- and long-term cognitive effects of chronic cannabinoids administration in late-adolescence rats. PLoS One 7 e31731 PMID: 22348124
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
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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 PMID: 22300105
Gibson et al (2008) TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons. Neuron 57 746 PMID: 18341994
Potenzieri et al (2008) The cannabinoid receptor agonist, WIN 55, 212-2, attenuates tumor-evoked hyperalgesia through peripheral mechanisms. Brain Res 1215 69 PMID: 18486111
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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
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
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
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
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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 PMID: 24027286
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
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Pinheiro et al (2016) Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin. Brain Res Bull 124 222 PMID: 27208730
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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 PMID: 27984180
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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 PMID: 20305287
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Farkas et al (2010) Retrograde endocannabinoid signaling reduces GABAergic synaptic transmission to gonadotropin-releasing hormone neurons. J Biomol Screen 151 5818 PMID: 20926585
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 PMID: 30002493
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
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
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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 PMID: 21859823
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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 PMID: 21744421
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Narushima et al (2007) Tonic enhancement of endocannabinoid-mediated retrograde suppression of inhibition by cholinergic interneuron activity in the striatum. J Neurosci 27 496 PMID: 17234582
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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 PMID: 17475795
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