CAS NO: | 119630-94-3 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
生物活性 | Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypicκ3-opioid receptoragonist, and a partial agonist at the clonedμandδ opioid receptors, and an antagonist atopioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect[1][2][3]. | ||||||||||||
IC50& Target | κ3-opioid receptor; μ- and δ-opioid receptors; Opioid-like NOP receptors[1][2] | ||||||||||||
体外研究 (In Vitro) | At the mu-opioid receptor (MOR), Naloxone benzoylhydrazone stimulates [35S]GTPγS binding (pEC50=8.59) and inhibits cyclic AMP accumulation (pEC50=8.74) with maximal effects (Emax) corresponding to 55 and 65% of those obtained with the MOR agonist DAMGO, respectively[1]. | ||||||||||||
体内研究 (In Vivo) | Analgesic studies in mice examining increasing doses of Naloxone benzoylhydrazone with a fixed dose of morphine reveals a biphasic curve. Naloxone benzoylhydrazone at doses as low as 1 μg/kg partially antagonized morphine analgesia. Higher Naloxone benzoylhydrazone doses continued to inhibit morphine analgesia in a dose-dependent manner, with the 1-mg/kg dose antagonizing completely morphine analgesia. As the Naloxone benzoylhydrazone dose increased beyond 1 mg/kg analgesia returned. Naloxone benzoylhydrazone also prduces a similar analgesic response when administered alone in mice and also is active in rats. Naloxone benzoylhydrazone has excellent p.o. activity, with an analgesic potency in mice equivalent to s.c. administration. In addition to blocking morphine analgesia, low doses of Naloxone benzoylhydrazone also partially reverses the inhibition of gastrointestinal transit in mice produced by morphine, antagonizes completely morphine lethality and precipitates withdrawal in morphine-dependent mice[4]. | ||||||||||||
分子量 | 445.51 | ||||||||||||
性状 | Solid | ||||||||||||
Formula | C26H27N3O4 | ||||||||||||
CAS 号 | 119630-94-3 | ||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||
储存方式 |
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