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ZM 241385 is a potent and highly selective Adenosine A2A-R antagonist, with a pA2 of 9.02 for Adenosine A2A-R in cardiac vasculature and selectivities of 1000, 91 and 500,000 over Adenosine A1-R, Adenosine A2B-R and
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Image Search Results
Journal: The International Journal of Neuropsychopharmacology
Article Title: mGlu5 and adenosine A2A receptor interactions regulate the conditioned effects of cocaine
doi: 10.1017/s146114571100126x
Figure Lengend Snippet: Fig. 2. Effect of MTEP treatment on A2A receptor binding in wild-type (WT) brain slices visualized by [125I]ZM241385. Representative autoradiograms of [125I]ZM241385 binding in (a) untreated and (b) MTEP pretreated WT mice (Bregma 0.86 mm). (c) Representative autoradiogram of non-specific binding (Bregma 0.86 mm). (d) Densitometric measurements of [125I]ZM241385 binding (dpm/mm2) in the striatum of untreated (WT) and MTEP-treated sections from WT mice. Data are expressed as mean of means (¡S.E.M.); * p<0.05 compared to untreated group (unpaired t test, n=5 per group). Cx, Cortex; St, striatum; Tu, olfactory tubercle. Scale bar, 0.55 mm.
Article Snippet: The
Techniques: Binding Assay
Journal: Neurourology and Urodynamics
Article Title: Adenosine Receptor Mechanisms Underlying Bladder Dysfunction in Male Rats With Bladder Outlet Obstruction
doi: 10.1002/nau.70080
Figure Lengend Snippet: Representative CMG traces of male BOO rats with intravesical drug administration of CCPA (A), ZM241385 (B), or Inosine (C). In each figure, the upper and lower traces showed CMG recordings during saline instillation and after intravesical drug treatment, respectively. CCPA or inosine did not have any effects on CMG parameters; however, ZM241385 significantly decreased the number of non‐voiding contractions (NVCs). The scatter plot of NVC rates using individual animal's data (D) showed that all animals had similar changes in bladder activity in response to each drug administration.
Article Snippet: For adenosine receptor modulation, CCPA (adenosine A1 receptor agonist; Tocris Bioscience, Minneapolis, USA),
Techniques: Saline, Activity Assay
Journal: PLoS ONE
Article Title: Oral Methylthioadenosine Administration Attenuates Fibrosis and Chronic Liver Disease Progression in Mdr2−/− Mice
doi: 10.1371/journal.pone.0015690
Figure Lengend Snippet: As indicated in the figure serum-starved murine monocyte/macrophages RAW 264.7 cells were pre-treated for 30 min with the A2A receptor antagonist ZM 241385 (10 µM) or the A2B receptor antagonist MRS 1754 (1 µM), then MTA or the adenosine receptor agonist NECA (20 µM) where added to the cultures for another 30 min. Subsequently and where indicated cells were treated with LPS (50 ng/ml) for up to 5 h. TNFα mRNA levels in cell lysates (A) and TNFα protein contents in conditioned media (B) were measured. * P <0.01 vs control, ** P <0.01 vs LPS, # P <0.05 vs LPS. The expression of the adenosine A2B receptor was measured in RAW 264.7 cells pre-treated with MTA or the adenosine agonist NECA (20 µM) for 30 min and then where indicated with LPS (50 ng/ml) for up to 5 h (C). * P <0.01 vs control, ** P <0.01 vs LPS.
Article Snippet: The adenosine receptor agonist 5′-(N-Ethylcarboxamido) adenosine (NECA) and the adenosine A2B receptor antagonist MRS 1754 were from Sigma, the
Techniques: Control, Expressing
Journal: BioMed research international
Article Title: The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance through Interleukin 6.
doi: 10.1155/2020/2603873
Figure Lengend Snippet: Figure 2: X-ray results of the effect of the adenosine A2A receptor agonist on fracture healing. The X-rays were taken in the front and rear position and lateral position. The image of 5 mm above and below the fracture line was captured using Photoshop software. The images were imported into IPP software for analysis. Red represents bone mineralized tissue, and green represents callus tissue. The area of callus tissue in the anterior and posterior and lateral positions was calculated as callus tissue + bone mineralized tissue area. The results show that the adenosine A2A receptor agonist could significantly increase the callus tissue area (callus tissue + bone mineralized tissue area) on the X line at 4, 6, and 8 weeks after modeling in rats, and the difference was statistically si gnificant (∗p < 0:05).
Article Snippet: Then, 5mg CGS 21680 (specific adenosine A2A receptor agonist; Selleck, USA) or ZM 241385 (
Techniques: Software
Journal: BioMed research international
Article Title: The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance through Interleukin 6.
doi: 10.1155/2020/2603873
Figure Lengend Snippet: Figure 3: CT image of the adenosine A2A receptor agonist on promoting fracture healing. A CT scan was performed on 200 layers above and below the fracture line. The data were imported into NRecon 1.6.10.2 for two-dimensional reconstruction. After reconstruction, the data were put into Mimics research 20.00 for 3D reconstruction. The bone mineralized tissues were marked with red and callus tissues with yellow. Callus formation was observed from the anteroposterior, lateral, and axial positions. The adenosine A2A receptor agonist is shown to promote callus formation.
Article Snippet: Then, 5mg CGS 21680 (specific adenosine A2A receptor agonist; Selleck, USA) or ZM 241385 (
Techniques: Computed Tomography
Journal: BioMed research international
Article Title: The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance through Interleukin 6.
doi: 10.1155/2020/2603873
Figure Lengend Snippet: Figure 5: Results of IL-6 immunohistochemistry. The results showed that the adenosine A2A receptor agonist could reduce the expression of IL-6 in the fracture area, while the adenosine A2A receptor inhibitor could increase the expression of IL-6.
Article Snippet: Then, 5mg CGS 21680 (specific adenosine A2A receptor agonist; Selleck, USA) or ZM 241385 (
Techniques: Immunohistochemistry, Expressing
Journal: BioMed research international
Article Title: The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance through Interleukin 6.
doi: 10.1155/2020/2603873
Figure Lengend Snippet: Figure 7: Effects of the adenosine A2A receptor agonist on Treg cells and Th17 cells in the blood of fracture rats. Flow cytometry showed that the adenosine A2A receptor agonist could reduce the proportion of Th17 cells in the blood of all CD4+ cells and increase the proportion of Treg cells in the blood of all CD4+ cells in the blood of rats at 1, 2, and 4 weeks after modeling. The adenosine A2A receptor inhibitor can increase the proportion of Th17 cells in the blood of all CD4+ cells and decrease the proportion of Treg cells in the blood of all CD4+ cells. The difference was statistically significant (∗p < 0:05).
Article Snippet: Then, 5mg CGS 21680 (specific adenosine A2A receptor agonist; Selleck, USA) or ZM 241385 (
Techniques: Flow Cytometry
Journal: BioMed research international
Article Title: The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance through Interleukin 6.
doi: 10.1155/2020/2603873
Figure Lengend Snippet: Figure 8: Effect of IL-6 on the adenosine A2A receptor agonist regulating the Treg and Th17 cells in the blood of bone fracture rats. It was found that IL-6 could reverse the adenosine A2A receptor agonist and increase the proportion of Treg cells and Th17 cells in all blood CD4+ cells in bone fracture rats at 1, 2, and 4 weeks. The difference was statistically significant (∗p < 0:05).
Article Snippet: Then, 5mg CGS 21680 (specific adenosine A2A receptor agonist; Selleck, USA) or ZM 241385 (
Techniques:
Journal: BioMed research international
Article Title: The Adenosine A2A Receptor Agonist Accelerates Bone Healing and Adjusts Treg/Th17 Cell Balance through Interleukin 6.
doi: 10.1155/2020/2603873
Figure Lengend Snippet: Figure 10: A brief diagram of the mechanism of the adenosine A2A receptor agonist promoting tibial fracture healing in rats. The adenosine A2A receptor agonist enters the tissue through the fibrin gel sustained release system. This reduces IL-6 levels in the blood and local tissues of the fracture, thus promoting fracture healing and regulating the Treg and Th17 cells.
Article Snippet: Then, 5mg CGS 21680 (specific adenosine A2A receptor agonist; Selleck, USA) or ZM 241385 (
Techniques: