Valorphin (Valorphin TFAsalt) has opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM.

μ opioid:14 nM

在体内模型中（雌性BLRB小鼠皮下接种同源乳腺癌细胞），同时用25 mg/m(2)的epirubicin和1 mg/kg的valorphin处理，与阴性对照组相比，肿瘤生长抑制率为42%，与仅用epirubicin处理的组相比，抑制率为22%（治疗第20天）。治疗开始26天后，生存率显著提高（与仅用epirubicin治疗的组相比，69%对39%）[1]。

49 mice were randomized in 4 groups: two groups (12 animals each) corresponding to the negative control, the reference group (13 animals) and the experimental group (12 animals). The control and the reference group were treated as in preliminary experiment, the experimental group were injected with the mixture of valorphin (1 mg/kg) and epirubicin (25 mg/m^2), dissolved in 0.9% NaCl solution in distilled water. Three injections (volume 0.2 ml) were made with 6-day intervals. Since no reliable difference in tumor size or lifespan of animals in the two negative control groups were observed, the data obtained in these groups were pooled. At day 20 after the first injection, the size of the tumors were determined as described above. Tumor volumes were calculated using for- mula, inhibition of tumor growth was determined using formula . Percentages of survival were determined for 1-26 days of treatment. The observation was quitted after the total death of the animals in the negative control group[1].