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Submit ReviewPPADS tetrasodium salt is a non-selective P2 purinergic antagonist. Blocks recombinant P2X1, P2X2, P2X3, P2X5 (IC50 = 1 - 2.6 μM), native P2Y2-like (IC50 ~ 0.9 mM), and recombinant P2Y4 (IC50 ~ 15 mM) receptors. PPADS tetrasodium salt delays onset of calcium responses to mild hypoosmotic stress in cortical slices. PPADS tetrasodium salt blocks P2X7 and reduces clinical and histological graft-versus-host disease development in a humanised mouse model.
2'5'-isomer also available.
分子量 | 599.3 |
公式 | C14H10N3Na4O12PS2 |
储存 | Desiccate at -20°C |
CAS Number | 192575-19-2 |
PubChem ID | 101086948 |
InChI Key | KURWUCJJNVPCHT-UHFFFAOYSA-J |
Smiles | [Na+].[Na+].[Na+].[Na+].CC1=C(O)C(C=O)=C(COP([O-])([O-])=O)C(\N=N\C2=C(C=C(C=C2)S([O-])(=O)=O)S([O-])(=O)=O)=N1 |
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 | |||
water | 100 |
以下数据基于产品分子量 599.3。 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 | 1.67 mL | 8.34 mL | 16.69 mL |
5 mM | 0.33 mL | 1.67 mL | 3.34 mL |
10 mM | 0.17 mL | 0.83 mL | 1.67 mL |
50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
参考文献是支持产品生物活性的出版物。
Ziganshin et al (1994) Selective antagonism by PPADS at P2x-purinoceptors in rabbit isolated blood vessels. Br.J.Pharmacol. 111 923 PMID: 8019770
Lambrecht et al (1992) PPADS, a novel functionally selective antagonist of P2 purinoceptor-mediated responses. Eur.J.Pharmacol. 217 217 PMID: 1330591
McLaren et al (1994) Investigation of the actions of PPADS, a novel P2x-purinoceptor antagonist, in the guinea-pig isolated vas deferens. Br.J.Pharmacol. 111 913 PMID: 8019769
Ralevic and Burnstock (1998) Receptors for purines and pyrimidines. Pharmacol.Rev. 50 413 PMID: 9755289
Thrane et al (2011) Critical role of aquaporin-4 (AQP4) in astrocytic Ca2+ signaling events elicited by cerebral edema. Proc.Natl.Acad.Sci.U S A 108 846 PMID: 21187412
Cuthbertson et al (2021) P2X7 receptor antagonism increases regulatory T cells and reduces clinical and histological graft-versus-host disease in a humanised mouse model. Clin.Sci. 135 495 PMID: 33463682
If you know of a relevant reference for PPADS tetrasodium salt, please let us know.
关键词: PPADS tetrasodium salt, PPADS tetrasodium salt supplier, P2, purinergic, antagonists, P2X, Receptors, Purinergic, P2Y, purinoceptors, antagonises, inhibitors, inhibits, 0625, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PPADS tetrasodium salt 的部分引用包括:
Cheung et al (2015) Pharmacological and molecular characterization of functional P2 receptors in rat embryonic cardiomyocytes. J Mol Neurosci 11 127 PMID: 25510459
Zhang et al (2016) Signaling mechanism for modulation by ATP of glycine receptors on rat retinal ganglion cells. Sci Rep 6 28938 PMID: 27357477
Yamashita et al (2016) Duloxetine inhibits microglial P2X4 receptor function and alleviates neuropathic pain after peripheral nerve injury PLoS One 11 e0165189 PMID: 27768754
Gómez-Gonzalo et al (2010) An excitatory loop with astrocytes contributes to drive neurons to seizure threshold. PLoS Biol 8 e1000352 PMID: 20405049
Rodríguez-Zayas et al (2012) Blockade of P2 nucleotide receptors after spinal cord injury reduced the gliotic response and spared tissue. Neuropsychopharmacology 46 167 PMID: 21647706
Pozner et al (2015) Intracellular calcium dynamics in cortical microglia responding to focal laser injury in the PC::G5-tdT reporter mouse. Front Mol Neurosci 8 12 PMID: 26005403
Fonseca et al (2015) Diadenosine tetraphosphate contributes to CB-induced tear secretion. Purinergic Signal 11 87 PMID: 25398705
Kouzaki et al (2011) The danger signal, extracellular ATP, is a sensor for an airborne allergen and triggers IL-33 release and innate Th2-type responses. J Immunol 186 4375 PMID: 21357533
Thrane et al (2011) Critical role of aquaporin-4 (AQP4) in astrocytic Ca2+ signaling events elicited by cerebral edema. Proc Natl Acad Sci U S A 108 846 PMID: 21187412
Miguel Cruz & Beall (2020) Extracellular ATP Increases Glucose Metabolism in Skeletal Muscle Cells in a P2 Receptor Dependent Manner but Does Not Contribute to Palmitate-Induced Insulin Resistance. Front Physiol 11 567378 PMID: 33101053
Bulavina et al (2013) NTPDase1 activity attenuates microglial phagocytosis. Purinergic Signal 9 199 PMID: 23208703
Cuthbertson et al (2021) P2X7 receptor antagonism increases regulatory T cells and reduces clinical and histological graft-versus-host disease in a humanised mouse model. Clin.Sci. 135 495 PMID: 33463682
McEwan et al (2021) Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation Life Sci 283 119850 PMID: 34314735
Coddou et al (2019) Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor. Neurosci Lett 690 219 PMID: 30366010
Conley (2017) Imaging extracellular ATP with a genetically-encoded, ratiometric fluorescent sensor. PLoS One 12 e0187481 PMID: 29121644
Mungenast (2011) Diacylglycerol signaling underlies astrocytic ATP release. Neural Plast 2011 537659 PMID: 21826278
Ievglevskyi et al (2012) Modulation of ATP-induced LTP by cannabinoid receptors in rat hippocampus. Purinergic Signal 8 705 PMID: 22453905
Zhong et al (2001) Multiple P2X receptors on guinea-pig pelvic ganglion neurons exhibit novel pharmacological properties. Br J Pharmacol 132 221 PMID: 11156581
Liu et al (1999) Rat chromaffin cells lack P2X receptors while those of the guinea-pig express a P2X receptor with novel pharmacology. Br J Pharmacol 128 61 PMID: 10498835
Gao et al (1999) Evidence that the ATP-induced increase in vasomotion of guinea-pig mesenteric lymphatics involves an endothelium-dependent release of thromboxane A2. Br J Pharmacol 127 1597 PMID: 10455315
Dowd et al (1998) P2X receptor-mediated excitation of nociceptive afferents in the normal and arthritic rat knee joint. Br J Pharmacol 125 341 PMID: 9786507
Neal et al (1998) Modulation of extracellular GABA levels in the retina by activation of glial P2X-purinoceptors. Br J Pharmacol 124 317 PMID: 9641548
Zhong et al (1998) Pharmacological and molecular characterization of P2X receptors in rat pelvic ganglion neurons. Br J Pharmacol 125 771 PMID: 9831914
Dowd et al (1998) Adenosine A1 receptor-mediated excitation of nociceptive afferents innervating the normal and arthritic rat knee joint. Br J Pharmacol 125 1267 PMID: 9863656
Takata and Hirase Cortical layer 1 and layer 2/3 astrocytes exhibit distinct calcium dynamics in vivo. PLoS One 3 e2525 PMID: 18575586
Kennedy et al (2007) Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder. J Neurosci 27 845 PMID: 17251425
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Study calcium oscillations using Fura2-AM in neuronal cultures at 10 micromolar concentration.
used to abrogate P2X responses, worked as expected.