MRS 1191

Names

[ Name ]:
MRS 1191

[Synonym ]:
5-Benzyl 3-ethyl 2-methyl-6-phenyl-4-(phenylethynyl)-1,4-dihydropyridine-3,5-dicarboxylate
3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2-methyl-6-phenyl-4-(2-phenylethynyl)-, 3-ethyl 5-(phenylmethyl) ester
mrs1191
5-Benzyl 3-ethyl 2-methyl-6-phenyl-4-(phenylethynyl)-1,4-dihydro-3,5-pyridinedicarboxylate

Biological Activity

[Description]:

MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells[1].

[Target]

Ki: 31.4 nM (human A3 adenosine receptor)[1]

[In Vitro]

The effects of putative A3 adenosine receptor antagonist of MRS-1191 is characterized in receptor binding and functional assays. MRS-1191 is found to be competitive in saturation binding studies using the agonist radioligand [125I]AB-MECA (N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide) at cloned human brain A3 receptor expressed in HEK-293 cells. Antagonism is 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-1191 with a KB value of 92 nM, proves to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase[1].

[References]

[1]. Jacobson KA, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
643.1±55.0 °C at 760 mmHg

[ Melting Point ]:
155 - 156 ℃

[ Molecular Formula ]:
C₃₁H₂₇NO₄

[ Molecular Weight ]:
477.550

[ Flash Point ]:
342.7±31.5 °C

[ Exact Mass ]:
477.194000

[ PSA ]:
64.63000

[ LogP ]:
7.16

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.639

[ Storage condition ]:
-20 °C

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

ATP releases ATP or other nucleotides from human peripheral blood leukocytes through purinergic P2 receptors.

Life Sci. 145 , 85-92, (2016)

Almost every eukaryotic cell releases ATP under certain conditions. The idea that ATP induces the release of ATP has been scantly investigated.We explored this possibility by assessing the rate of exo...

The infarct-sparing effect of IB-MECA against myocardial ischemia/reperfusion injury in mice is mediated by sequential activation of adenosine A3 and A 2A receptors.

Basic Res. Cardiol. 110(2) , 16, (2015)

Conflicting results exist regarding the role of A3 adenosine receptors (A3ARs) in mediating cardioprotection during reperfusion following myocardial infarction. We hypothesized that the effects of the...

Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.

Neuropharmacology 36 , 1157-1165, (1997)

The effects of putative A3 adenosine receptor antagonists of three diverse chemical classes (the flavonoid MRS 1067, the 6-phenyl-1,4-dihydropyridines MRS 1097 and MRS 1191, and the triazoloquinazolin...

Related Compounds

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