MRS 2179 tetrasodium salt
Chemical Name: 2'-Deoxy-N6-methyladenosine 3',5'-bisphosphate tetrasodium salt
Biological ActivityMRS 2179 tetrasodium salt is a competitive antagonist at P2Y1 receptors (KB = 100 nM). Selective over P2X1 (IC50 = 1.15 μM), P2X3 (IC50 = 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors. Inhibits the upregulation of NTPDase1 by ATPγS.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells.
Lu et al.
Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y1 receptor ligands.
Nandanan et al.
Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate.
Boyer et al.
Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.
Nandanan et al.
Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors.
Brown et al.
Drug Dev.Res., 2000;49:253
Citations for MRS 2179 tetrasodium salt
The citations listed below are publications that use Tocris products. Selected citations for MRS 2179 tetrasodium salt include:
35 Citations: Showing 1 - 10
Trypanosoma cruzi Infection Induces Pannexin-1 Channel Opening in Cardiac Myocytes.
Authors: Barría Et al.
Am J Trop Med Hyg 2018;98:105
Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells.
Cell Signal 2018;51:59
Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells.
Authors: Kleiner Et al.
Mol Vis 2018;24:647
A complementary role for tetraspanin superfamily member TSSC6 and ADP purinergic P2Y12 receptor in platelets.
Thromb Res 2017;161:12
Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X1, P2X2, P2X3 channels, P2Y and A3 metabotropic receptors in neurotransmission.
Authors: Liñán-Rico Et al.
Pannexin channels mediate the acquisition of myogenic commitment in C2C12 reserve cells promoted by P2 receptor activation.
Authors: Riquelme Et al.
J Neurosci 2015;3:25
Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors.
Authors: Kawano Et al.
PLoS One 2015;10:e0127919
Anti-platelet therapy with clopid. prevents endothelial dysfunction and vascular remodeling in aortas from hypertensive rats.
Authors: Giachini Et al.
PLoS One 2014;9:e91890
Nucleolin down-regulation is involved in ADP-induced cell cycle arrest in S phase and cell apoptosis in vascular endothelial cells.
Authors: Wang Et al.
PLoS One 2014;9:e110101
Lactate-mediated glia-neuronal signalling in the mammalian brain.
Authors: Tang Et al.
Nat Commun 2014;5:3284
Detection of platelet sensitivity to inhibitors of COX-1, P2Y1, and P2Y12 using a whole blood microfluidic flow assay.
Authors: Li and Diamond
Thromb Res 2014;133:203
Loss of calcium/calmodulin-dependent protein kinase II activity in cortical astrocytes decreases glutamate uptake and induces neurotoxic release of ATP.
Authors: Ashpole Et al.
J Biol Chem 2013;288:14599
Neurogenic mucosal bicarbonate secretion in guinea pig duodenum.
Authors: Fei Et al.
Br J Pharmacol 2013;168:880
Antagonism of P2Y1-induced vasorelaxation by acyl CoA: a critical role for palmitate and 3'-phosphate.
Authors: Alefishat Et al.
Br J Pharmacol 2013;168:1911
Pharmacodynamic interplay of the P2Y(1), P2Y(12), and TxA(2) pathways in platelets: the potential of triple antiplatelet therapy with P2Y(1) receptor antagonism.
Authors: Oestreich Et al.
Thromb Res 2013;131:e64
Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation.
Authors: Pinheiro Et al.
Cell Commun Signal 2013;11:70
Investigation of the functional expression of purine and pyrimidine receptors in porcine isolated pancreatic arteries.
Authors: Alsaqati Et al.
Purinergic Signal 2013;10:241
Constitutively released adenosine diphosphate regulates proplatelet formation by human megakaryocytes.
Authors: Balduini Et al.
Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter.
Authors: Duffy Et al.
Neurogastroenterol Motil 2012;24:e41
Purinergic receptors are required for HIV-1 infection of primary human macrophages.
Authors: Hazleton Et al.
J Immunol 2012;188:4488
Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits.
Authors: Martín-Gil Et al.
Br J Pharmacol 2012;165:1163
Adenylate cyclase 5 coordinates the action of ADP, P2Y1, P2Y13 and ATP-gated P2X7 receptors on axonal elongation.
Authors: Puerto Et al.
J Cell Sci 2012;125:176
DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia.
Authors: Begum Et al.
J Neurochem 2012;120:622
Multiscale prediction of patient-specific platelet function under flow.
Authors: Flamm Et al.
Dynamic mass redistribution assays decode surface influence on signaling of endogenous purinergic P2Y receptors.
Authors: Tran Et al.
Assay Drug Dev Technol 2012;10:37
Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia.
Authors: Kuboyama Et al.
Front Cell Dev Biol 2011;31:1930
Facilitation of transmitter release from rat sympathetic neurons via presynaptic P2Y(1) receptors.
Authors: Chandaka Et al.
Br J Pharmacol 2011;164:1522
β-nicotinamide adenine dinucleotide is an enteric inhibitory neurotransmitter in human and nonhuman primate colons.
Authors: Hwang Et al.
Autocrine and paracrine roles for ATP and serotonin in mouse taste buds.
Authors: Huang Et al.
Cancer Med 2009;29:13909
Purinergic and nitrergic junction potential in the human colon.
Authors: Gallego Et al.
Am J Physiol Gastrointest Liver Physiol 2008;295:G522
Purinergic activation of anion conductance and osmolyte efflux in cultured rat hippocampal neurons.
Authors: Li and Olson
Am J Physiol Cell Physiol 2008;295:C1550
Residual platelet ADP reactivity after clopid. treatment is dependent on activation of both the unblocked P2Y(1) and the P2Y (12) receptor and is correlated with protein expression of P2Y (12).
Authors: Braun Et al.
Purinergic Signal 2007;3:195
Beta-nicotinamide adenine dinucleotide is an inhibitory neurotransmitter in visceral smooth muscle.
Authors: Mutafova-Yambolieva Et al.
Proc Natl Acad Sci U S A 2007;104:16359
PAR4, but not PAR1, signals human platelet aggregation via Ca2+ mobilization and synergistic P2Y12 receptor activation.
Authors: Holinstat Et al.
J Biol Chem 2006;281:26665
Differential effects of P2Y1 and P2Y12 nucleotide receptors on ERK1/ERK2 and phosphatidylinositol 3-kinase signalling and cell proliferation in serum-deprived and nonstarved glioma C6 cells.
Authors: Czajkowski Et al.
Br J Pharmacol 2004;141:497
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used to block P2Y1 receptor mediated calcium entry in mouse astrocytes stimulated with 2MeSADP