Naloxone benzoylhydrazone - CAS:119630-94-3

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Naloxone benzoylhydrazone (Synonyms:NalBzoH)

目录号 : KM3354 CAS No. : 119630-94-3 纯度 : 98%

Data Sheet 产品使用指南

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 μ 和 δ 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。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock

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生物活性

Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.

IC₅₀&Target

κ3-opioid receptor; μ- and δ-opioid receptors; Opioid-like NOP receptors

体外研究

At the mu-opioid receptor (MOR), Naloxone benzoylhydrazone stimulates [S]GTPγS binding (pEC₅₀=8.59) and inhibits cyclic AMP accumulation (pEC₅₀=8.74) with maximal effects (E_max) corresponding to 55 and 65% of those obtained with the MOR agonist DAMGO, respectively.
At the κ-opioid receptor (KOR), Naloxone benzoylhydrazone stimulates [S]GTPγS binding (pEC₅₀=9.70) and inhibits cyclic AMP formation (pEC₅₀=9.45) .
In CHO cells expressing the δ-opioid receptor (DOR), Naloxone benzoylhydrazone increases [S]GTPγS binding (pEC₅₀=8.49) and inhibits cyclic AMP formation (pE₅₀=8.61).

体内研究

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.

分子式

C₂₆H₂₇N₃O₄

分子量

445.51

CAS号

119630-94-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： 98%

Data Sheet

产品使用指南

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。

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注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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动物实验计算换算器