MRS 1220

C₂₁H₁₄ClN₅O₂

403.82

MFCD01321046

24896720

NA.77

MRS1220 is a putative A3 adenosine receptor antagonist. MRS 1220 was found to be competitive in saturation binding studies using the agonist radioligand ¹²⁵I AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of ³⁵S guanosine 5′-O-(3-thiotriphosphate (³⁵S GTP-gamma-S) to the associated G-proteins. MRS 1220 and MRS 1191, with KB values of 1.7 and 92 nM, respectively, proved to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase. In addition, MRS 1220 reversed the effect of A3 agonist-elicited inhibition of tumor necrosis factor-alpha formation in the human macrophage U-937 cell line, with an IC₅₀ value of 0.3 μM.

This compound is featured on the Adenosine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

100

solid

white

DMSO: 2 mg/mL
2-hydroxypropyl-β-cyclodextrin: insoluble
H₂O: insoluble
ethanol: insoluble

Clc1ccc2nc(NC(=O)Cc3ccccc3)n4nc(nc4c2c1)-c5ccco5

1S/C21H14ClN5O2/c22-14-8-9-16-15(12-14)20-25-19(17-7-4-10-29-17)26-27(20)21(23-16)24-18(28)11-13-5-2-1-3-6-13/h1-10,12H,11H2,(H,23,24,28)

TWWFAXQOKNBUCR-UHFFFAOYSA-N

human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)

5, 25 mg in glass bottle

11 - Combustible Solids

WGK 3

Eyeshields, Gloves, type N95 (US)