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Naloxone benzoylhydrazone

CAS No. : 119630-94-3

MCE 站：Naloxone benzoylhydrazone

产品活性：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 具有有效的镇痛作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

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 (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 [³⁵S]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 [³⁵S]GTPγS binding (pEC₅₀=8.49) ａnd inhibits cyclic AMP formation (pE₅₀=8.61).

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.

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