Description
MRS1706 is a selective adenosine A
2B receptor inverse agonist with K
i values of 1.39, 157, 112, and 230 nM for human A
2B, A
1, A
2A, and A
3 receptors, respectively.
Uses
MRS 1706 is a selective and potent Adenosine A2B-R inverse agonist Ki (binding affinity) values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.
Biological Activity
Potent and selective adenosine A 2B receptor inverse agonist (K i values are 1.39, 157, 112 and 230 nM for human A 2B , A 1 , A 2A and A 3 receptors respectively).
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: | Ada–/– mice[2] |
| Dosage: | 1 and 10 μM |
| Administration: | Intracavernous injection |
| Result: | Inhibited A2BR signaling and reduced the magnitude and duration.
Inhibited the level of cAMP.
|
References
[1] YONG-CHUL KIM. Anilide Derivatives of an 8-Phenylxanthine Carboxylic Congener Are Highly Potent and Selective Antagonists at Human A2B Adenosine Receptors[J]. Journal of Medicinal Chemistry, 2000, 43 6: 1165-1172. DOI:
10.1021/jm990421v[2] QILAN LI. ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320 2: 637-645. DOI:
10.1124/jpet.106.111203
