144313-54-2
144313-54-2 结构式
基本信息
Valorphin TFAsalt
VAL-VAL-TYR-PRO-TRP-THR-GLN
H-VAL-VAL-TYR-PRO-TRP-THR-GLN-OH
Valorphin H-Val-Val-Tyr-Pro-Trp-Thr-Gln-OH
L-Glutamine, L-valyl-L-valyl-L-tyrosyl-L-prolyl-L-tryptophyl-L-threonyl-
物理化学性质
常见问题列表
IC50: 14 nM (mu-opioid receptor), 200 nM (δ-opioid receptor)
Valorphin is a derivative of dihydrovaltrate with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC 50 of 14 nM. Valorphin has low affinity for δ-opioid receptor (IC 50 , 200 nM) and shows no affinity for κ receptor (IC 50 , >10 μM). Valorphin (>10 μM) decreases spontaneous firing rate of cerebellar rat Purkinje cells. Valorphin (1 μM) treatment 48 h prior to 0.1 μM epirubicin, or 0.1 μM vincristine, or 0.05 μM vincristine, causes 100% tumor cell death.
Valorphin exhibits pronounced analgesic activity in mice, rats and rhesus monkeys via s.c, with ED 50 s of ≤5.2 mg/kg, but barely active after oral administration. Valorphin (1 mg/kg) causes 42% of tumor growth inhibition in female BLRB mice bearing syngeneic mammary carcinoma cells.