MIPS521 functions as a positive allosteric modulator of the adenosine A1 receptor (A1AR), with a lower allosteric affinity for A1R (pKB=4.95; KB=11 μM). It demonstrates analgesic effects in vivo by modulating elevated levels of endogenous adenosine [1][2].
体内研究
MIPS521 (1-30 μg in 10 μL; intrathecal administration) reverses mechanical hyperalgesia in rats, providing robust antinociception [2].
MIPS521 (10 μg in 10 μL; administered intrathecally) significantly alleviates spontaneous pain in a conditioned place preference model [2].
MIPS521 (1-30 μg in 10 μL; administered intrathecally) decreases eEPSCs in the spinal cord of nerve-injured rats, exhibiting a pEC50 of 6.9. The magnitude of MIPS521-induced reduction in synaptic current amplitude is significantly higher in nerve-injured rats compared to sham surgery controls [2].
MIPS521 (0.3-30 μM; pretreatment for 10 min, co-treatment for 30 min) induces a concentration-dependent enhancement of adenosine (ADO) signaling in a cAMP inhibition assay in CHO cells, expressed as a percentage of the inhibition caused by 3 μM forskolin-mediated cAMP [2].
搜索
