Description
MRS1523 is a selective adenosine A
3 receptor antagonist (K
is = 18.9 and 113 nM for human and rat A
3 receptors, respectively,
versus K
is = 15.6 and 2.05 μM for rat A
1 and A
2A receptors, respectively). As activation of the A
3 receptor is linked to several second messenger systems for signaling pathways involving inflammatory, asthmatic, and ischemic responses, this selective antagonist may be useful in characterizing the various functions of the receptor.
Uses
MRS 1523 is a selective A3 adenosine receptor (A3AR) antagonist in human and rat.
Biochem/physiol Actions
MRS 1523 is a selective?adenosine A3 receptor antagonist in the rat.
in vitro
mrs1523 reversed the increase in mrna expression in b16-f10 melanoma cells. also, mrs1523 antagonized the modulation in the expression level of the proteins, which indicated that adenosine a3r mediated the responses [1].
in vivo
c57bl/6j, male mice, inoculated b16-f10 melanoma cells, were administered mrs1523 at a dose of 100 μg/kg orally twice daily for 15 days. mrs1523 counteracted the activity of ib-meca which is an adenosine a3r agonist. in addition, it was demonstrated that the response was adenosine a3r mediated. the modulation of up-regulation of gsk-3β expression level was neutralized by mrs1523, further suggesting the specificity of the response [1].
References
[1]. madi, l., rosenberg-haggen, b., nyska, a., & korenstein, r. enhancing pigmentation via activation of a3 adenosine receptors in b16 melanoma cells and in human skin explants. experimental dermatology. 2012; 22(1): 74-77.
