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Naloxone benzoylhydrazone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Naloxone benzoylhydrazone图片
CAS NO:119630-94-3
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品名称
NalBzoH
产品介绍
Naloxone benzoylhydrazone (NalBzoH) 是一种混合的激动剂/拮抗剂。Naloxone benzoylhydrazone 是原型κ3-阿片样受体激动剂,是克隆的μδ阿片样受体的部分激动剂,在阿片样NOP受体上是拮抗剂。Naloxone benzoylhydrazone 可用于缓解疼痛的研究。
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].
At the κ-opioid receptor (KOR), Naloxone benzoylhydrazone stimulates [35S]GTPγS binding (pEC50=9.70) and inhibits cyclic AMP formation (pEC50=9.45)[1].
In CHO cells expressing the δ-opioid receptor (DOR), Naloxone benzoylhydrazone increases [35S]GTPγS binding (pEC50=8.49) and inhibits cyclic AMP formation (pE50=8.61)[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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month