| Bioactivity | MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction[1][2]. | ||||||||||||
| Target | Ki: 1.39 (human A2B receptor), 112 (human A2A receptor), 157 (human A1 receptor), 230 nM (human A3 receptor) | ||||||||||||
| Invitro | MRS-1706 (0.1-5 μM) has antagonist effect of NECA on the wild-type adenosine A2B 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 A2B 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]. Animal Model: | ||||||||||||
| Name | MRS-1706 | ||||||||||||
| CAS | 264622-53-9 | ||||||||||||
| Formula | C27H29N5O5 | ||||||||||||
| Molar Mass | 503.55 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Li Q, et, al. ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor. J Pharmacol Exp Ther. 2007 Feb;320(2):637-45. [2]. Mi T, et, al. Excess adenosine in murine penile erectile tissues contributes to priapism via A2B adenosine receptor signaling. J Clin Invest. 2008 Apr;118(4):1491-501. |