1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Naloxone benzoylhydrazone

Naloxone benzoylhydrazone (Synonyms: NalBzoH)

Cat. No.: HY-107743 Purity: >99.0%
Handling Instructions

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.

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Naloxone benzoylhydrazone Chemical Structure

Naloxone benzoylhydrazone Chemical Structure

CAS No. : 119630-94-3

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Description

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[1][2][3].

IC50 & Target

κ3-opioid receptor; μ- and δ-opioid receptors; Opioid-like NOP receptors[1][2]

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].

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].

Molecular Weight

445.51

Formula

C₂₆H₂₇N₃O₄

CAS No.

119630-94-3

SMILES

O[[email protected]]12[[email protected]@]34C5=C(C(O)=CC=C5C[[email protected]@]2([H])N(CC=C)CC4)O[[email protected]@]3([H])/C(CC1)=N/NC(C6=CC=CC=C6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

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

Purity: >99.0%

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Keywords:

Naloxone benzoylhydrazoneNalBzoHOpioid ReceptorAnalgesiaκ3-Opioidμ-Opioidδ-OpioidNOPorallyactiveInhibitorinhibitorinhibit

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Naloxone benzoylhydrazone
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