Naloxazone

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Naloxazone
File:Naloxazone.png
style="background: #F8EABA; text-align: center;" colspan="2" | Identifiers
CAS number 73674-85-8
PubChem 9576788
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style="background: #F8EABA; text-align: center;" colspan="2" | Properties
Molecular formula C19H23N3O3
Molar mass 341.4 g mol−1
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
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.

See also

References

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  1. Pasternak GW, Childers SR, Snyder SH. "Opiate analgesia: evidence for mediation by a subpopulation of opiate receptors." Science. 1980 May 2; 208(4443):514-6. PMID 6245448. doi:10.1126/science.6245448
  2. Ling GS, Simantov R, Clark JA, Pasternak GW. Naloxonazine actions in vivo. European Journal of Pharmacology. 1986 Sep 23;129(1-2):33-8. PMID 3021478