Naloxazone

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Not to be confused with Naloxone.
Naloxazone
Naloxazone.svg
Names
IUPAC name
(5α)-17-Allyl-3,14-dihydroxy-4,5-epoxymorphinan-6-one hydrazone
Other names
Naloxone- 6-hydrazone
Identifiers
73674-85-8 YesY
ChEMBL ChEMBL354010 YesY
Jmol 3D model Interactive image
PubChem 9576788
  • C=CCN1CCC23C4C(=NN)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O
Properties
C19H23N3O3
Molar mass 341.40422 g/mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
YesY verify (what is YesYN ?)
Infobox references

Naloxazone is an irreversible μ-opioid receptor antagonist which is selective for the μ1 receptor subtype.[1] Naloxazone produces very long lasting antagonist effects as it forms a covalent bond to the active site of the mu-opioid receptor,[2] thus making it impossible for the molecule to unbind and blocking the receptor permanently until the receptor is recycled by endocytosis.

It has been reported that naloxazone is unstable in acidic solution, dimerizing into the more stable and much more potent antagonist naloxonazine.[3] Under conditions in which no naloxonazine formation could be detected, naloxazone did not display irreversible μ opioid receptor binding.[3]

See also

References

  1. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ 3.0 3.1 Lua error in package.lua at line 80: module 'strict' not found.


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