adenosine a2a receptor a2ar antagonist sch58261  (MedChemExpress)

Journal: Bioactive Materials

Article Title: Immunomodulatory supramolecular hydrogel for rheumatoid arthritis management via adenosine A2A receptor-mediated macrophage remodeling

doi: 10.1016/j.bioactmat.2025.11.031

Figure Lengend Snippet: The design of an inflammatory macrophages-targeted, acid-sensitive PNSH for delivery MTX and its role in promoting A2AR activation on M2 macrophages for arthritis therapy. (A)The structure of acid-sensitive polymer-nanomedicine supramolecular hydrogels, composed of drug-loaded MTX NPs. (B) Schematic illustration of arthritis therapy targeting inflammatory joint network via mPECN NPs-mediated release of MTX. This approach leverages MTX targeting the A2AR and repolarization of macrophages from the pro-inflammatory M1 phenotype to the anti-inflammatory M2 phenotype. Activation of A2AR and macrophage repolarization by mPECN-MTX NPs synergistically enhanced the anti-inflammatory effect of PNSH-mediated nanomedicine in an arthritis rat model.

Article Snippet: The selective adenosine A2A receptor (A2AR) antagonist SCH58261 (HY-19533) was purchased from MedChemExpress (Shanghai, China).

Techniques: Activation Assay, Polymer

Journal: Bioactive Materials

Article Title: Immunomodulatory supramolecular hydrogel for rheumatoid arthritis management via adenosine A2A receptor-mediated macrophage remodeling

doi: 10.1016/j.bioactmat.2025.11.031

Figure Lengend Snippet: MTX@PNSH promotes anti-inflammatory M2 macrophages through the A2AR signaling pathway. (A) The intracellular cAMP levels in Raw 264.7 cells were determined by homogeneous time-resolved fluorescence (HTRF) following different treatments. (B) qRT-PCR analysis of relative mRNA of A2ar with different treatments. (C) Immunostaining of A2AR expression in Raw 264.7 cells with different treatments. (D) Flow cytometry analysis of A2AR + cells in Raw 264.7 cells with different treatments and the percentage of A2AR + cells in Raw 264.7 cells with different treatments. (E) qRT-PCR analysis of relative mRNA expression of Pdl1 without LPS treatment. (F) qRT-PCR analysis of relative mRNA expression of Ido1 without LPS treatment. (G) qRT-PCR analysis of relative mRNA expression of Pdl1 with LPS treatment. (H) qRT-PCR analysis of relative mRNA expression of Ido1 with LPS treatments. (I) Western blotting analysis of A2AR protein level in macrophages after 24 h of different treatment with or without A2AR inhibitor. (J) Quantitative analysis of A2AR protein level in different treatments with or without A2AR inhibitor. (K) Flow cytometry analysis of CD11b and CD39 in Raw 264.7 cells with different treatments and the percentage of CD11b + CD39 + macrophages. (L) Flow cytometry analysis of CD11b and CD73 in Raw 264.7 cells with different treatments and the percentage of CD11b + CD73 + macrophages. (M) Flow cytometry analysis of CD11b and PD-L1 in Raw 264.7 cells after 24 h of different treatments and the percentage of CD11b + PD-L1 + macrophages in Raw 264.7 cells after 24 h of different treatments. Data are presented as mean ± SD, n = 3. Statistical significance was determined using one-way ANOVA, followed by Dunnett's post hoc test for comparisons between groups.

Article Snippet: The selective adenosine A2A receptor (A2AR) antagonist SCH58261 (HY-19533) was purchased from MedChemExpress (Shanghai, China).

Techniques: Fluorescence, Quantitative RT-PCR, Immunostaining, Expressing, Flow Cytometry, Western Blot

Journal: Frontiers in Pharmacology

Article Title: Adenosine A 2A receptors regulate D 2 -type medium spiny neurons in the nucleus accumbens to mediate pain and depression comorbidity

doi: 10.3389/fphar.2026.1759544

Figure Lengend Snippet: A 2A Rs modulated the excitability of D 2 -MSNs in the NAcS (A) Timeline of the stereotactic injection and ex vivo electrophysiology (B) Typical micrograph showing the electrophysiological recording of mCherry-labeled NAcS D 2 -MSNs, scale bar = 10 µm (C) Sample of whole-cell recording of action potentials in the NAcS after 0.1 µM CGS 21680 perfusion (D) (left) 0.1 µM CGS 21680 perfusion increased the number of eAPs of mCherry-labeled neurons (right) The minimal voltage threshold to induce eAPs was lower after perfusion with 0.1 µM CGS 21680 (n = 9 cells from 4 mice) (E) Sample of whole-cell recording of action potentials in the NAcS after 0.1 µM SCH 58261 perfusion (F) (left) 0.1 µM SCH 58261 perfusion decreased the number of eAPs of mCherry-labeled neurons (right) The minimal voltage threshold to induce eAPs was higher after perfusion with 0.1 µM SCH 58261 (n = 12 cells from 4 mice) Data are shown as mean ± s.e.m. , ** P < 0.01, *** P < 0.001.

Article Snippet: The A 2A R agonist CGS 21680 (MedChemExpress, HY-13201A) and antagonist SCH 58261 (MedChemExpress, HY-19533) were initially dissolved in 100% dimethyl sulfoxide (DMSO) to prepare 10 mM stock solutions and stored at −20 °C.

Techniques: Injection, Ex Vivo, Labeling

Journal: Frontiers in Pharmacology

Article Title: Adenosine A 2A receptors regulate D 2 -type medium spiny neurons in the nucleus accumbens to mediate pain and depression comorbidity

doi: 10.3389/fphar.2026.1759544

Figure Lengend Snippet: NAcS A 2A Rs antagonism alleviated SNI-induced pain-depression comorbidity (A) Timeline of cannula and SNI surgery, intracerebral injection, Von Frey and Hargreaves tests at specified time points (B,C) 50%PWTs (B) and PWL (C) in mice treated with vehicle or SCH 58261 (4 ng/side) 1 W following SNI surgery (n = 8 mice/group) (D–F) 50% PWTs (D) , PWL (E) , and immobile time in the FST (F) after a single microinjection of vehicle or SCH 58261 (4 ng/side) 6 W following SNI surgery (n = 8 mice/group) (G–I) 50% PWTs (G) , PWL (H) , and immobile time in the FST (I) after five consecutive microinjections of vehicle or SCH 58261 (4 ng/side) 6 W following SNI surgery (n = 8 mice/group). Data are represented as mean ± s.e.m. , * P < 0.05, ** P < 0.01, *** P < 0.001, ns means no significance.

Article Snippet: The A 2A R agonist CGS 21680 (MedChemExpress, HY-13201A) and antagonist SCH 58261 (MedChemExpress, HY-19533) were initially dissolved in 100% dimethyl sulfoxide (DMSO) to prepare 10 mM stock solutions and stored at −20 °C.

Techniques: Injection, Microinjection