| Description | Valorphin TFA(144313-54-2(free base)) is a semisynthetic derivative of dihydrovaltrate with opioid analgesic activity |
| In vitro | 在体外利用大鼠和豚鼠的脑组织匀浆进行结合研究显示，该化学化合物更偏好μ-受体位点。通过对培养的小脑Purkinje细胞进行浴液应用，抑制了其自发性放电，这与吗啡的效果相似。在小鼠的热板和尾巴摆动测试中，以及大鼠的Randall-Selitto测试中，已证明该化合物具有镇痛活性。在恒河猴中，valorphin表现出自我给药行为，但对纳洛酮的挑战只引起轻微的撤退迹象。Valorphin是一种新型化学实体，其结构与已知的阿片类化合物无关，且优先与阿片μ受体相互作用[1]。 |
| Synonyms | Valorphin TFA(144313-54-2(free bas)) |
| molecular weight | 1006.03 |
| Molecular formula | C46H62F3N9O13 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10.06 mg/mL (10 mM) |
| References | 1. Maurer R , R?Mer D , H.H. Büscher, et al. Valorphin: A novel chemical structure with opioid activity[J]. Neuropeptides, 1985, 5(4-6):387-390. 2. Smith W D . A COMPARISON IN MICE OF NALOXONE AND NALORPHINE AS ANTAGONISTS TO NEUROLEPTANALGESIC DRUGS[J]. BJA: British Journal of Anaesthesia(11):11. |