ZM 241385

Cat. No. 1036

ZM 241385 C16H15N7O2 [139180-30-6]

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Chemical Name: 4-(2-[7-Amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol

Biological Activity

Potent and highly selective A2A adenosine antagonist, with a pA2 of 9.02 for A2A receptors in guinea pig cardiac vasculature and selectivities of 1000, 91 and 500,000 over A1, A2B and A3 sites respectively. Active in vivo.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data

M.Wt:
337.34
Formula:
C16H15N7O2
Solubility:
Soluble to 5 mM in ethanol and to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at RT
CAS No:
139180-30-6

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

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Keddie et al (1996) In vivo characterisation of ZM 241385, a selective adenosine A2A receptor antagonist. Eur.J.Pharmacol. 301 107. PMID: 8773453.

Poucher et al (1996) Pharmacodynamics of ZM 241385, a potent A2a adenosine receptor antagonist, after enteric administration in rat, cat and dog. J.Pharm.Pharmacol. 48 601. PMID: 8832494.

Poucher et al (1995) The in vitro pharmacology of ZM 241385, a potent, non-xanthine, A2a selective adenosine receptor antagonist. Br.J.Pharmacol. 115 1096. PMID: 7582508.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for ZM 241385 include:

Caiazzo et al (2016) Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide. Biochem.Pharmacol. 112 72. PMID: 27188793.

Oliveira et al (2015) Deficits in endogenous adenosine formation by ecto-5'-nucleotidase/CD73 impair neuromuscular transmission and immune competence in experimental autoimmune myasthenia gravis. Mediators Inflamm 2015 460610. PMID: 25691808.

Perez-Aso et al (2015) Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther 17 249. PMID: 26370839.

Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661. PMID: 26030448.

Ahsan and Mehal (2014) Activation of adenosine receptor A2A increases HSC proliferation and inhibits death and senescence by down-regulation of p53 and Rb. Front Pharmacol 5 69. PMID: 24782773.

Chiodi et al (2014) Cocaine-induced changes of synaptic transmission in the striatum are modulated by adenosine A2A receptors and involve the tyrosine phosphatase STEP. Neuropsychopharmacology 39 569. PMID: 23989619.

Perígolo-Vicente et al (2014) IL-6, A1 and A2aR: a crosstalk that modulates BDNF and induces neuroprotection. Biochem Biophys Res Commun 449 477. PMID: 24845382.

Welihinda and Amento et al (2014) Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation. J Inflamm (Lond) 11 37. PMID: 25473378.

He et al (2013) Adenosine regulates bone metabolism via A1, A2A, and A2B receptors in bone marrow cells from normal humans and patients with multiple myeloma. FASEB J 27 3446. PMID: 23682121.

Nam et al (2013) Adenosine transporter ENT1 regulates the acquisition of goal-directed behavior and ethanol drinking through A2A receptor in the dorsomedial striatum. J Neurosci 33 4329. PMID: 23467349.

Kinsey et al (2012) Autocrine adenosine signaling promotes regulatory T cell-mediated renal protection. J Am Soc Nephrol 23 1528. PMID: 22835488.

Lee et al (2012) When cytokinin, a plant hormone, meets the adenosine A2A receptor: a novel neuroprotectant and lead for treating neurodegenerative disorders? PLoS One 7 e38865. PMID: 22719969.

Mediero et al (2012) Adenosine A2A receptor activation prevents wear particle-induced osteolysis. Sci Transl Med 4 135ra65. PMID: 22623741.

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.

Suzuki et al (2012) CD8+CD45RA+CCR7+FOXP3+ T cells with immunosuppressive properties: a novel subset of inducible human regulatory T cells. J Immunol 189 2118. PMID: 22821963.

Tozzi et al (2012) A2A adenosine receptor antagonism enhances synaptic and motor effects of cocaine via CB1 cannabinoid receptor activation. PLoS One 7 e38312. PMID: 22715379.

Williams and Cronstein (2012) The effect of A(2A) adenosine receptor activation on C-C chemokine receptor 7 expression in human THP1 macrophages during inflammation. Inflammation 35 614. PMID: 21739164.

Jin et al (2011) Paeoniflorin suppresses the expression of intercellular adhesion molecule-1 (ICAM-1) in endotoxin-treated human monocytic cells. Br J Pharmacol 164 694. PMID: 21542832.

Ruiz-García et al (2011) Cooperation of adenosine with macrophage Toll-4 receptor agonists leads to increased glycolytic flux through the enhanced expression of PFKFB3 gene. J Biol Chem 286 19247. PMID: 21464136.

Zhukov et al (2011) Biophysical mapping of the adenosine A2A receptor. J Med Chem 54 4312. PMID: 21661720.

Bingham et al (2010) A2A adenosine receptor stimulation decreases foam cell formation by enhancing ABCA1-dependent cholesterol efflux. J Leukoc Biol 87 683. PMID: 20089670.

Gazoni et al (2010) Activation of A1, A2A, or A3 adenosine receptors attenuates lung ischemia-reperfusion injury. J Thorac Cardiovasc Surg 140 440. PMID: 20398911.

Gebremedhin et al (2010) Adenosine can mediate its actions through generation of reactive oxygen species. J Cereb Blood Flow Metab 30 1777. PMID: 20531463.

Himer et al (2010) Adenosine A2A receptor activation protects CD4+ T lymphocytes against activation-induced cell death. FASEB J 24 2631. PMID: 20371613.

Mandapathil et al (2010) Generation and accumulation of immunosuppressive adenosine by human CD4+CD25highFOXP3+ regulatory T cells. J Biol Chem 285 7176. PMID: 19858205.

Riccioni et al (2010) Adenosine A(2A) Receptor Binding Profile of Two Antagonists, ST1535 and KW6002: Consideration on the Presence of Atypical Adenosine A(2A) Binding Sites. Front Psychiatry 1 22. PMID: 21423433.

Alam et al (2009) A2A adenosine receptor (AR) activation inhibits pro-inflammatory cytokine production by human CD4+ helper T cells and regulates Helicobacter-induced gastritis and bacterial persistence. Mucosal Immunol 2 232. PMID: 19262506.

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.

Wilson et al (2009) The A2B adenosine receptor impairs the maturation and immunogenicity of dendritic cells. J Immunol 182 4616. PMID: 19342636.

Csóka et al (2008) Adenosine A2A receptor activation inhibits T helper 1 and T helper 2 cell development and effector function. FASEB J 22 3491. PMID: 18625677.

Chan et al (2006) Adenosine A(2A) receptors play a role in the pathogenesis of hepatic cirrhosis. Br J Pharmacol 148 1144. PMID: 16783407.

Jacobson et al (2005) A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists. Chem Biol 12 237. PMID: 15734651.

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.

Germack and Dickenson (2004) Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. Br J Pharmacol 141 329. PMID: 14751870.

Wen and Knowles (2003) Extracellular ATP and adenosine induce cell apoptosis of human hepatoma Li-7A cells via the A3 adenosine receptor. Br J Pharmacol 140 1009. PMID: 14530217.

Hirsh and Silinsky (2002) Inhibition of spontaneous acetylcholine secretion by 2-chloroadenosine as revealed by a protein kinase inhibitor at the mouse neuromuscular junction. Br J Pharmacol 135 1897. PMID: 11959792.

Avila et al (2001) A(1)-, A(2A)- and A(3)-subtype adenosine receptors modulate intraocular pressure in the mouse. Br J Pharmacol 134 241. PMID: 11564641.

Nieri et al (2001) Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO. Br J Pharmacol 134 745. PMID: 11606314.

Slesinger (2001) British Pharmacological Society Meeting. 18-21 December 2000, University of Birmingham. Abstracts. Br J Pharmacol 133 Suppl 1P. PMID: 11403025.

Guibert et al (1998) Dependence of P2-nucleotide receptor agonist-mediated endothelium-independent relaxation on ectonucleotidase activity and A2A-receptors in rat portal vein. Br J Pharmacol 123 1732. PMID: 9605582.

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Keywords: ZM 241385, supplier, Potent, selective, A2A, antagonist, Receptors, adenosines, ZM241385, AstraZeneca, Tocris Bioscience, A2A Receptor Antagonist products

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