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Constitutive and functional expression of runt-related transcription factor-2 by microglial cells
2014, Neurochemistry InternationalCitation Excerpt :The increase by ATP was significantly prevented by the prior addition of the general P2 receptor antagonist PPADS, the P2X receptor antagonist iso-PPADS and the P2X7 receptor (P2X7R) antagonist oxATP, respectively (Fig. 5B). The antagonistic properties are reported as follows: <PPADS> P2X1, P2X2, P2X3 and P2X5 (IC50 = 1–2.6 μM), P2Y2 (IC50 = ∼0.9 mM), P2Y4 (IC50 = ∼15 mM) (Lambrecht et al., 1992; McLaren et al., 1994; Ralevic and Burnstock, 1998; Ziganshin et al., 1994); <iso-PPADS> pKi = 6.5 (Khakh et al., 1994); <oxATP> (IC50 = 30 μM) (Murgia et al., 1993). In BV-2 cells, moreover, a significant increase in Runx2 levels was seen after the exposure to the selective P2X7R agonist BzATP (BzATP: EC50 = 285 ± 16 μM, ATP: EC50 = 936 ± 21) (Young et al., 2007) at 300 μM (Fig. 5C).
Enzymatic activity of cholesterol oxidase immobilized onto polymer nanoparticles mediated by Congo red
2013, Colloids and Surfaces B: BiointerfacesCitation Excerpt :Desorption experiments indicated changes of less than 5% in the QCR values, evidencing high affinity between CR molecules and PS/PEG particles. Considering that the adsorption takes place at pH 7and that the pKb of CR is 4.6 ± 0.2 [31], the amount of CR protonated amine group is small, but might be enough to bind to the sulfate groups on the particle surface and to increase the ζ-potential values from - (70 ± 4) mV up to - (46 ± 2) mV. Moreover, H bonding between the CR uncharged amine groups and PEG oligomers on the particle surface might favor the adsorption.
Vas deferens - A model used to establish sympathetic cotransmission
2010, Trends in Pharmacological SciencesisoPPADS
2007, xPharm: The Comprehensive Pharmacology ReferenceStructure-activity relationships of novel P2-receptor antagonists structurally related to Reactive Blue 2
2005, European Journal of Medicinal ChemistryCitation Excerpt :All 19 compounds, 15 of which for the first time, investigated in the present study antagonized P2-receptor mediated responses, either in RVD or in GPTC or in both whole tissue preparations. Contraction of the RVD elicited by the ecto-nucleotidase resistant agonist α,β-meATP is mediated by the cloned P2X1-receptor [37–44]. Eigh of the 19 tested anthraquinone derivatives administered in concentrations of up to 100 μM antagonized the effect of α,β-meATP (Table 1).
The novel heteromeric bivalent ligand SB9 potently antagonizes P2Y<inf>1</inf> receptor-mediated responses
2000, Journal of the Autonomic Nervous System