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说明： Selective A1 antagonist
化学名： 8-Cyclopentyl-1,3-dipropylxanthine
纯度： ≥99% (HPLC)
生物活性 for DPCPX
DPCPX is a potent and selective A1 adenosine receptor antagonist, both in vitro and in vivo. Ki values are 3.9, 130, 50 and 4000 nM for human A1, A2A, A2B and A3 receptors respectively.
技术数据 for DPCPX
| 分子量 | 304.39 |
| 公式 | C16H24N4O2 |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 102146-07-6 |
| PubChem ID | 1329 |
| InChI Key | FFBDFADSZUINTG-UHFFFAOYSA-N |
| Smiles | CCCN1C2=C(N=C(N2)C2CCCC2)C(=O)N(CCC)C1=O |
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.
溶解性数据 for DPCPX
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 1.52 | 5 温和加热 | |
| ethanol | 3.04 | 10 温和加热 |
制备储备液 for DPCPX
以下数据基于产品分子量 304.39。 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 |
|---|---|---|---|
| 0.1 mM | 32.85 mL | 164.26 mL | 328.53 mL |
| 0.5 mM | 6.57 mL | 32.85 mL | 65.71 mL |
| 1 mM | 3.29 mL | 16.43 mL | 32.85 mL |
| 5 mM | 0.66 mL | 3.29 mL | 6.57 mL |
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产品说明书 for DPCPX
参考文献 for DPCPX
参考文献是支持产品生物活性的出版物。
Canals et al (2008) Metabolic challenge to glia activates and adenosine-mediated safety mechanism that promotes neuronal survival by delaying the onset of spreading depression waves. J.Cereb.Blood Flow Metab. 28 1835 PMID: 18612316
Klotz (2000) Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch.Pharmacol. 362 382 PMID: 11111832
Kuan et al (1992) An experimental paradigm for investigating the role of endogenous adenosine/A1 receptor interactions in vivo. J.Pharmacol.Exp.Ther. 263 657 PMID: 1432696
Von der Leyen (1989) Effects of 1,3-dipropyl-8-cyclopentylxanthine (DPCPX), a highly selective adenosine receptor antagonist, on force of contraction in guinea-pig atrial and ventricular cardiac preparations. Naunyn Schmiedebergs Arch.Pharmacol. 340 204 PMID: 2554151
If you know of a relevant reference for DPCPX, please let us know.
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关键词: DPCPX, DPCPX supplier, A1, selective, antagonists, Receptors, adenosines, Adenosine, 0439, Tocris Bioscience
45 篇 DPCPX 的引用文献
引用文献是使用了 Tocris 产品的出版物。 DPCPX 的部分引用包括：
Kaster et al (2013) The antidepressant-like effect of inosine in the FST is associated with both adenosine A1 and A 2A receptors. Purinergic Signal 9 481 PMID: 23613131
Diógenes et al (2014) Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase. Cereb Cortex 24 67 PMID: 22997174
Kan et al (2012) Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol 86 10338 PMID: 22787201
Stoddart et al (2012) Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay. Chem Biol 19 1105 PMID: 22999879
Aitta-Aho et al (2012) Importance of GluA1 subunit-containing AMPA glutamate receptors for mor. state-dependency. PLoS One 7 e38325 PMID: 22675452
Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285 PMID: 22368777
Hensler et al (2012) GABAB receptor-positive modulators: brain region-dependent effects. J Pharmacol Exp Ther 340 19 PMID: 21954301
Burbassi et al (2010) Alterations of CXCR4 function in μ-opioid receptor-deficient glia. Eur J Neurosci 32 1278 PMID: 20880358
Liu et al (2018) Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect. Brain Res. 1700 47 PMID: 29935155
Lee et al (2012) Polyphenol (-)-epigallocatechin gallate-induced cardioprotection may attenuate ischemia-reperfusion injury through adenosine receptor activation: a preliminary study. J Cell Biol 63 340 PMID: 23115687
Long et al (2010) Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine. Proc Natl Acad Sci U S A 335 781 PMID: 20855445
Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661 PMID: 26030448
Augusto et al (2013) Ecto-5'-nucleotidase (CD73)-mediated formation of adenosine is critical for the striatal adenosine A2A receptor functions. Biochim Biophys Acta 33 11390 PMID: 23843511
Lutz et al (2011) Sequential and opposing alterations of 5-HT(1A) receptor function during withdrawal from chronic mor. Eur Neuropsychopharmacol 21 835 PMID: 21402471
Carlsen and Perrier (2014) Purines released from astrocytes inhibit excitatory synaptic transmission in the ventral horn of the spinal cord. Front Neural Circuits 8 60 PMID: 24926236
Li et al (2014) Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina. Vis Neurosci 31 237 PMID: 24844306
Fuss et al (2013) Hippocampal serotonin-1A receptor function in a mouse model of anxiety induced by long-term voluntary wheel running. Synapse 67 648 PMID: 23505009
Rex et al (2009) Different Rho GTPase-dependent signaling pathways initiate sequential steps in the consolidation of long-term potentiation. Am J Respir Crit Care Med 186 85 PMID: 19596849
Yu et al (2009) Effect of ventilation pressure on alveolar fluid clearance and β-agonist responses in mice. Neuropsychopharmacology 297 L785 PMID: 19684202
Bhanu et al (2008) Inhibition of erythroblast growth and fetal hemoglobin production by ribofuranose-substituted adenosine derivatives. PLoS One 1782 504 PMID: 18586086
Eckle et al (2008) A2B adenosine receptor signaling attenuates acute lung injury by enhancing alveolar fluid clearance in mice. J Neurosci 118 3301 PMID: 18787641
Wolk et al (2008) Influenza A virus inhibits alveolar fluid clearance in BALB/c mice. Am J Physiol Regul Integr Comp Physiol 178 969 PMID: 18689466
Burbassi et al (2008) GTPgammaS incorporation in the rat brain: a study on mu-opioid receptors and CXCR4. J Neuroimmune Pharmacol 3 26 PMID: 18247130
Ruby et al (2014) Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light. Korean J Anesthesiol 39 2432 PMID: 24755889
Mioranzza et al (2011) Blockade of adenosine A(1) receptors prevents methylphenidate-induced impairment of object recognition task in adult mice. Prog Neuropsychopharmacol Biol Psychiatry 35 169 PMID: 21044657
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
Epperson et al (2009) Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts. Am J Physiol Cell Physiol 296 C1171 PMID: 19244482
Xi et al (2009) Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol 47 684 PMID: 19695259
Clark et al (2009) Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation. J Neurosci 29 11237 PMID: 19741130
Park et al (2012) A1 adenosine receptor allosteric enhancer PD-81723 protects against renal ischemia-reperfusion injury. Am J Physiol Renal Physiol 303 F721 PMID: 22759398
Ilie et al (2012) Adenosine release during seizures attenuates GABAA receptor-mediated depolarization. J Neurosci 32 5321 PMID: 22496577
Maeda and Koos (2009) Adenosine A1 and A2a receptors modulate Insemia, glycemia, and lactatemia in fetal sheep. Purinergic Signal 296 R693 PMID: 19118101
Angelantonio et al (2015) Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R. J Inflamm (Lond) 9 409 PMID: 26528137
Kohno et al (2015) Anti-inflammatory effects of adenosine N1-oxide. Am J Physiol Lung Cell Mol Physiol 12 2 PMID: 25632271
Cunha et al (2015) Creatine, similarly to KA, affords antidepressant-like effects in the tail suspension test via adenosine A1 and A2A receptor activation. J Clin Invest 11 215 PMID: 25702084
Dobson et al (2015) Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling. J Neurosci 10 e0125974 PMID: 25933382
Scianni et al (2013) Fractalkine (CX3CL1) enhances hippocampal N-MthD.-aspartate receptor (NMDAR) function via D-serine and adenosine receptor type A2 (A2AR) activity. J Neuroinflammation 10 108 PMID: 23981568
Thakkar et al (2010) Role of wake-promoting basal forebrain and adenosinergic mechanisms in sleep-promoting effects of ethanol. Alcohol Clin Exp Res 34 997 PMID: 20374215
Yang et al (2010) Adenosine mediated desensitization of cAMP signaling enhances T-cell responses. Eur J Immunol 40 449 PMID: 19950175
Moore et al (2003) Adenosine gates synaptic plasticity at hippocampal mossy fiber synapses. J Neurosci 100 14397 PMID: 14608033
Kornerup et al (2005) Pharmacological characterisation of the adenosine receptor mediating increased ion transport in the mouse isolated trachea and the effect of allergen challenge. Br J Pharmacol 144 1011 PMID: 15685200
Melyan et al (2004) Metabotropic regulation of intrinsic excitability by synaptic activation of kainate receptors. J Neurosci 24 4530 PMID: 15140923
Satake et al (2006) Characterization of AMPA receptors targeted by the climbing fiber transmitter mediating presynaptic inhibition of GABAergic transmission at cerebellar interneuron-Purkinje cell synapses. J Neurosci 26 2278 PMID: 16495455
Rex et al (2005) Long-term potentiation is impaired in middle-aged rats: regional specificity and reversal by adenosine receptor antagonists. J Neurosci 25 5956 PMID: 15976084
Newman (2005) Calcium increases in retinal glial cells evoked by light-induced neuronal activity. Front Cell Neurosci 25 5502 PMID: 15944378
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A selective A1 receptor antagonist.
By
Anonymous on 02/06/2018
分析类型： Ex Vivo
种属： Rat
This a selective A1 receptor antagonist. We used at 100nM in rat brain slice.