MRS-1706

MRS-1706 is a potent and selective adenosine A_2B receptor inverse agonist. MRS-1706 has K_i values of 1.39, 112, 157, and 230 nM for human A_2B, A_2A, A₁ and A₃ receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction^[1][2]. IC50 & Target: Ki: 1.39 (human A_2B receptor), 112 (human A_2A receptor), 157 (human A₁ receptor), 230 nM (human A₃ receptor)^[2] In Vitro: MRS-1706 (0.1-5 μM) has antagonist effect of NECA on the wild-type adenosine A_2B receptor in a dose-dependent manner^[1].
MRS-1706 (0.1-10000 nM) induces inhibition of yeast growth, which yeast cells expressing seven CAM adenosine A_2B receptors, with IC₅₀ values of 43, 54, 40, 98, 166, 133 nM for F84L, F84S, F84L/S95G, T42A, T42A/V54A, N36S/T42A, respectively^[1].
MRS-1706 (1 μM) inhibits the adenosine-mediated induction of cAMP in wild-type corpus cavernosal strips (CCSs) and decreases the level of cAMP^[2]. In Vivo: MRS-1706 (1-10 μM; intracavernous injection; Ada^–/– mice) reduces the magnitude and duration of electrical field stimulation (EFS)-induced contraction of corpus cavernosal strips (CCSs) from sickle cell disease (SCD) transgenic mice and inhibits the level of cAMP^[2].