difelikefalin hydrochloride

Difelikefalin HCl is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin HCl is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).

Difelikefalin-d5 (CR-845-d5) hydrochloride 是 Difelikefalin 的氘代物。Difelikefalin (CR-845) 是一种选择性的 κ 阿片受体 (KOR) 激动剂，具备抗炎作用，并在慢性肾脏病等疾病中用于调节瘙痒。