The A2B adenosine receptor (AR) is a member of the P1 family of seven-transmembrane ARs, and it couples to Gs to increase cAMP and Gq11 to increase (1,4,5)inositol triphosphate (IP3)/diacylglycerol (DAG). MRS 1754 is a selective antagonist ligand of A2BAR with Ki value of 1.97 nM[1]. 3H-MRS 1754 was shown to bind with high affinity to a single class of binding sites in membranes of HEK-293 cells expressing the human A2B receptor[2]. Finally, MRS 1754 inhibited the NECA-induced Ca2+ responses and cAMP production in a concentration-dependent manner. Treatment of the T24 cell line for 4h with NECA resulted in an increase in interleukin-8 production which was sensitive to the adenosine A2B antagonist MRS 1754[3].
MRS 1754 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human macrophages
10 nM
7 days
To evaluate the effect of MRS1754 on adenosine and/or TGF-β1-induced macrophage to myofibroblast transition. Results showed that MRS1754 treatment reduced adenosine/TGF-β1-induced myofibroblast marker expression and morphological changes.
Cells. 2020 Apr 23;9(4):1051
Rat-transformed enteric glial cells (EGCs)
0.1 μM
19 hours
MRS1754 reversed the inhibitory effects of BAY60-6583 on TLR4 expression and IL-1β release
Cells. 2020 May 18;9(5):1245
HEK293 cells
1 μmol/L
To investigate the effect of MRS 1754 on inosine-induced activation of adenylyl cyclase, results showed that MRS 1754 abolished the activation of adenylyl cyclase by inosine.
Hypertension. 2023 May;80(5):981-994
UMSCC47 cells
1 μM
72 hours
Under metabolic stress or cisplatin treatment conditions, MRS 1754 (A2BR antagonist) significantly reduced exosome production.
Purinergic Signal. 2020 Jun;16(2):231-240
HMEC-1 cells
10 µmol/L
24 hours
Inhibit A2B adenosine receptor, reduce VEGF and eNOS expression
Exp Biol Med (Maywood). 2015 Nov;240(11):1472-9
MRS 1754 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Streptozotocin-induced diabetic nephropathy model
Intraperitoneal injection
0.5 mg/kg/48 h
Every 48 hours for 8 weeks
To evaluate the effect of MRS1754 on glomerular fibrosis, macrophage infiltration, and macrophage-myofibroblast transition in diabetic nephropathy rats. Results showed that MRS1754 treatment attenuated glomerular fibrosis, reduced macrophage infiltration, and decreased macrophage-myofibroblast transition.
Cells. 2020 Apr 23;9(4):1051
C57BL/6 mice
High-fat diet-induced obesity model
In vitro organ bath
10 nM
Single administration, duration not specified
MRS1754 enhanced tachykininergic contractions in colonic preparations from HFD mice, an effect blunted by fluorocitrate
Cells. 2020 May 18;9(5):1245
Sprague-Dawley rats
Diabetic nephropathy model
Intraperitoneal injection
0.5 mg/kg/48 hours
Every 48 hours for 8 weeks
To evaluate the effect of MRS1754 on the expression of immune-related genes, infiltration of monocytes/macrophages, and M2 macrophage polarization in diabetic nephropathy rats. Results showed MRS1754 reduced the expression of immune-related genes, infiltration of monocytes/macrophages, and M2 macrophage polarization.
Int J Mol Sci. 2023 Jun 29;24(13):10829
Rabbits
Anesthetized rabbits
Intravenous
1 mg/kg
Single dose
To test the inhibitory effect of MRS1754 on ITI-214 cardiovascular responses
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