Cat. No. 0439
Chemical Name: 8-Cyclopentyl-1,3-dipropylxanthine
Biological ActivityPotent 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
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.
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Citations are publications that use Tocris products. Selected citations for DPCPX include:
Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661. PMID: 26030448.
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.
Aitta-Aho et al (2012) Importance of GluA1 subunit-containing AMPA glutamate receptors for morphine 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.
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.
Lutz et al (2011) Sequential and opposing alterations of 5-HT(1A) receptor function during withdrawal from chronic morphine. Eur Neuropsychopharmacol 21 835. PMID: 21402471.
Burbassi et al (2010) Alterations of CXCR4 function in μ-opioid receptor-deficient glia. Eur J Neurosci 32 1278. PMID: 20880358.
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.
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.
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.
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.
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.
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Keywords: DPCPX, supplier, A1, selective, antagonists, Receptors, adenosines, Tocris Bioscience, A1 Receptor Antagonist products
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