212329-37-8 Usage
Description
MRS1523 is a selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 μM for rat A1 and A2A receptors, respectively). As activation of the A3 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.
Check Digit Verification of cas no
The CAS Registry Mumber 212329-37-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,1,2,3,2 and 9 respectively; the second part has 2 digits, 3 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 212329-37:
(8*2)+(7*1)+(6*2)+(5*3)+(4*2)+(3*9)+(2*3)+(1*7)=98
98 % 10 = 8
So 212329-37-8 is a valid CAS Registry Number.
InChI:InChI=1/C23H29NO3S/c1-5-12-17-19(23(26)28-8-4)18(7-3)24-21(16-13-10-9-11-14-16)20(17)22(25)27-15-6-2/h9-11,13-14H,5-8,12,15H2,1-4H3
212329-37-8Relevant articles and documents
A3 adenosine receptor antagonists
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, (2008/06/13)
Disclosed are pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of selectively blocking an A3adenosine receptor of a mammal by the use of one or more of these derivatives. An example of the pyridine derivative is of the formula (I): wherein R2is ethyl, R3is ethylsulfanyl; R4is ethyl, propyl, or hydroxypropyl; R5is ethyl, propyl, fluoroethyl, or fluoropropyl; and R6is phenyl or fluorophenyl. The derivatives of the present invention can be used for inhibiting binding of ligands to an adenosine receptor. The derivatives also can be used for characterizing an adenosine receptor.
