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Chemical Compound Review

AC1NSKQU     4-[2-[[4-amino-8-(2-furyl)- 1,3,5,7,9...

Synonyms: ZINC02572472, L000893
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Disease relevance of ZM241385


High impact information on ZM241385

  • Two-way MLR-stimulated T cell proliferation was reduced by ATL313, a selective A(2A)R agonist in a dose-responsive manner ( approximately 70%; 10 nM), an effect reversed by the A(2A)R antagonist ZM241385 (100 nM) [5].
  • Selective agonist (CGS21680) and antagonist (ZM241385) of A2A adenosine receptor were used in functional assays and cDNA probes for different sybtypes of adenosine receptors were used in Northern blot studies [6].
  • Pretreatment with ZM241385 (A(2A)-Ado receptor antagonist) alone or in combination with MRS1706 (A(2B)-Ado receptor antagonist) resulted in a pure constriction upon Ado, whereas 8-cyclopentyltheophylline (CPT) (A(1)-Ado receptor antagonist) inhibited the constrictor response [7].
  • The actions of caffeine (3.0, 10.0 and 30.0 mg/kg, i.p.), the A1 receptor antagonist DPCPX (1.0 and 3.0 mg/kg, i.p.) and the A2A receptor antagonist ZM241385 (0.5 and 1.0 mg/kg, i.p.) in relation to age-related effects on olfactory functions were also studied [8].
  • Inhibition of CD49d expression was equally inhibited by ATL146e, added before or after TNF priming, and was reversed by incubation with the A(2A)AR-selective antagonist 4-[2-[7-amino-2-(2-furyl) (1, 2, 4)triazolo(2,3-a) (1, 3, 5)triazin-5-yl-amino]ethyl]-phenol (ZM241385; 100 nM) [9].

Biological context of ZM241385


Anatomical context of ZM241385

  • In contrast, ZM241385 had no effect on the depressor response or the reduction in phrenic nerve activity evoked by aortic nerve stimulation [3].
  • We hypothesized that spinal cord functional and cytoarchitectural preservation from ATL-146e would be lost with simultaneous administration of the specific adenosine A(2A) antagonist ZM241385 (ZM), thus proving that adenosine A(2A) receptor activation is responsible for the protective effects of this compound [12].
  • Each experiment tested a specific dose of an A1 receptor antagonist (8-cyclopentyltheophylline given via microinjection into the basal forebrain), an A2a receptor antagonist (ZM241385 via intraperitoneal administration), or both [13].
  • Although ZM241385, a selective A(2A)R antagonist, significantly enhanced the increase in neutrophil elastase release and intracellular Ca(2+) concentrations in neutrophils stimulated with fMLP, this agent did not affect the endotoxin-induced TNF-alpha production by monocytes [14].
  • A total of 10 microM AMP579 reduced neutrophil adherence to thrombin-stimulated endothelium (neutrophils/mm(2)) from 269+/-16 to 44+/-4 (P<0.05); this was reversed by ZM241385, but not by DPCPX or MRS1220 [15].

Associations of ZM241385 with other chemical compounds

  • The nonselective AdoR antagonist xanthine amine congener (XAC), the A(2A)-selective antagonist ZM241385, the A(2B)-selective antagonists 3-N-propylxanthine (enprofylline) and 3-isobutyl-8-pyrrolidinoxanthine (IPDX), and the A(1)-selective antagonist cyclopentyl-1,3-dipropylxanthine (CPX) were used [16].
  • The A2a receptor antagonist, ZM241385 had mixed effects on DAMGO-mediated inhibition, producing either a further inhibition or a reversal of the inhibition [17].
  • Adenosine inhibited Fc epsilon RI-mediated tryptase release from HCMC in a dose-dependent manner, and this inhibitory effect was completely blocked by the A2a receptor antagonist ZM241385 [18].
  • Coronary vasodilatation by CGS21680 was inhibited bythe A2A receptor antagonist, 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo [2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol (ZM241385) [19].

Gene context of ZM241385


Analytical, diagnostic and therapeutic context of ZM241385


  1. Adenosine concentration in the porcine coronary artery wall and A2A receptor involvement in hypoxia-induced vasodilatation. Frøbert, O., Haink, G., Simonsen, U., Gravholt, C.H., Levin, M., Deussen, A. J. Physiol. (Lond.) (2006) [Pubmed]
  2. Ischaemic skeletal muscle hyperaemia in the anaesthetized cat: no contribution of A2A adenosine receptors. Poucher, S.M. J. Physiol. (Lond.) (1997) [Pubmed]
  3. Localization and action of adenosine A2a receptors in regions of the brainstem important in cardiovascular control. Thomas, T., St Lambert, J.H., Dashwood, M.R., Spyer, K.M. Neuroscience (2000) [Pubmed]
  4. Adenosine A(2A) receptors play a role in the pathogenesis of hepatic cirrhosis. Chan, E.S., Montesinos, M.C., Fernandez, P., Desai, A., Delano, D.L., Yee, H., Reiss, A.B., Pillinger, M.H., Chen, J.F., Schwarzschild, M.A., Friedman, S.L., Cronstein, B.N. Br. J. Pharmacol. (2006) [Pubmed]
  5. Activation of Adenosine 2A Receptors Attenuates Allograft Rejection and Alloantigen Recognition. Sevigny, C.P., Li, L., Awad, A.S., Huang, L., McDuffie, M., Linden, J., Lobo, P.I., Okusa, M.D. J. Immunol. (2007) [Pubmed]
  6. Memory of extracellular adenosine A2A purinergic receptor-mediated signaling in murine T cells. Koshiba, M., Kojima, H., Huang, S., Apasov, S., Sitkovsky, M.V. J. Biol. Chem. (1997) [Pubmed]
  7. Contribution of adenosine receptors in the control of arteriolar tone and adenosine-angiotensin II interaction. Lai, E.Y., Patzak, A., Steege, A., Mrowka, R., Brown, R., Spielmann, N., Persson, P.B., Fredholm, B.B., Persson, A.E. Kidney Int. (2006) [Pubmed]
  8. Caffeine reverses age-related deficits in olfactory discrimination and social recognition memory in rats. Involvement of adenosine A1 and A2A receptors. Prediger, R.D., Batista, L.C., Takahashi, R.N. Neurobiol. Aging (2005) [Pubmed]
  9. Activation of A2A adenosine receptors inhibits expression of alpha 4/beta 1 integrin (very late antigen-4) on stimulated human neutrophils. Sullivan, G.W., Lee, D.D., Ross, W.G., DiVietro, J.A., Lappas, C.M., Lawrence, M.B., Linden, J. J. Leukoc. Biol. (2004) [Pubmed]
  10. Adenosine A2A receptors regulate the extracellular accumulation of excitatory amino acids upon metabolic dysfunction in chick cultured retinal cells. Rego, A.C., Agostinho, P., Melo, J., Cunha, R.A., Oliveira, C.R. Exp. Eye Res. (2000) [Pubmed]
  11. A novel cell-based assay for G-protein-coupled receptor-mediated cyclic adenosine monophosphate response element binding protein phosphorylation. Selkirk, J.V., Nottebaum, L.M., Ford, I.C., Santos, M., Malany, S., Foster, A.C., Lechner, S.M. Journal of biomolecular screening : the official journal of the Society for Biomolecular Screening. (2006) [Pubmed]
  12. Functional and cytoarchitectural spinal cord protection by ATL-146e after ischemia/reperfusion is mediated by adenosine receptor agonism. Reece, T.B., Kron, I.L., Okonkwo, D.O., Laurent, J.J., Tache-Leon, C., Maxey, T.S., Ellman, P.I., Linden, J., Tribble, C.G., Kern, J.A. J. Vasc. Surg. (2006) [Pubmed]
  13. Effect of sleep deprivation on righting reflex in the rat is partially reversed by administration of adenosine A1 and A2 receptor antagonists. Tung, A., Herrera, S., Szafran, M.J., Kasza, K., Mendelson, W.B. Anesthesiology (2005) [Pubmed]
  14. Adenosine and selective A(2A) receptor agonists reduce ischemia/reperfusion injury of rat liver mainly by inhibiting leukocyte activation. Harada, N., Okajima, K., Murakami, K., Usune, S., Sato, C., Ohshima, K., Katsuragi, T. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  15. A novel adenosine analog, AMP579, inhibits neutrophil activation, adherence and neutrophil-mediated injury to coronary vascular endothelium. Nakamura, M., Zhao, Z.Q., Clark, K.L., Velez, D.V., Guyton, R.A., Vinten-Johansen, J. Eur. J. Pharmacol. (2000) [Pubmed]
  16. Adenosine receptor antagonists and retinal neovascularization in vivo. Mino, R.P., Spoerri, P.E., Caballero, S., Player, D., Belardinelli, L., Biaggioni, I., Grant, M.B. Invest. Ophthalmol. Vis. Sci. (2001) [Pubmed]
  17. Adenosine contributes to mu-opioid synaptic inhibition in rat substantia gelatinosa in vitro. Ackley, M.A., Baldwin, S.A., King, A.E. Neurosci. Lett. (2005) [Pubmed]
  18. Inhibitory effect of adenosine on degranulation of human cultured mast cells upon cross-linking of Fc epsilon RI. Suzuki, H., Takei, M., Nakahata, T., Fukamachi, H. Biochem. Biophys. Res. Commun. (1998) [Pubmed]
  19. Effects of adenosine receptor agonists on guinea-pig isolated working hearts and the role of endothelium and NO. Maddock, H.L., Broadley, K.J., Bril, A., Khandoudi, N. J. Pharm. Pharmacol. (2002) [Pubmed]
  20. Adenosine A2A receptors and depression. El Yacoubi, M., Costentin, J., Vaugeois, J.M. Neurology (2003) [Pubmed]
  21. Differential effect of insulin and elevated glucose level on adenosine handling in rat T lymphocytes. Pawelczyk, T., Sakowicz-Burkiewicz, M., Kocbuch, K., Szutowicz, A. J. Cell. Biochem. (2005) [Pubmed]
  22. Antagonism of coronary artery relaxation by adenosine A2A-receptor antagonist ZM241385. Arif Hasan, A.Z., Abebe, W., Mustafa, S.J. J. Cardiovasc. Pharmacol. (2000) [Pubmed]
  23. Role of endothelium in ischaemia-induced myocardial dysfunction of isolated working hearts: cardioprotection by activation of adenosine A(2A) receptors. Maddock, H.L., Broadley, K.J., Bril, A., Khandoudi, N. Journal of autonomic pharmacology. (2001) [Pubmed]
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