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nalmexone

Structure via PubChem · Public domain (PubChem)

EntityQ6961001· pop 6· linked from 694 articles

Nalmexone (INN; also known as nalmexone hydrochloride (USAN) or by the development codes EN-1620A and UM-592) is a semisynthetic, opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties that was never marketed. In clinical studies it was found to have comparable analgesic efficacy to morphine, though with several-fold reduced potency. In addition, nalmexone's side effects, the most common of which were sleepiness and sweating, were reported to be similar to those of morphine, albeit with a noticeably higher degree of incidence.

Chemical data

Formula
C21H25NO4
Molecular weight
355.4 g/mol
IUPAC name
(4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-(3-methylbut-2-enyl)-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one

via PubChem

Drug data · ChEMBL

Max clinical phase
Phase 2
Molecule type
Small molecule

via ChEMBL · EBI

Wikidata facts

Mass
355.178
Show 4 more facts
chemical formula
C₂₁H₂₅NO₄
canonical SMILES
CC(=CCN1CCC23C4C(=O)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O)C
isomeric SMILES
CC(=CCN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O)C
different from
naltrexone
Sources (3)

via Wikidata · CC0

~1 min read

Encyclopedic overview

3 sections
Contents
  • Synthesis
  • See also
  • References

Nalmexone (INN; also known as nalmexone hydrochloride (USAN) or by the development codes EN-1620A and UM-592) is a semisynthetic, opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties that was never marketed. In clinical studies it was found to have comparable analgesic efficacy to morphine, though with several-fold reduced potency. In addition, nalmexone's side effects, the most common of which were sleepiness and sweating, were reported to be similar to those of morphine, albeit with a noticeably higher degree of incidence.

==Synthesis== Nalmexone can be synthesized from oxymorphone: 700px|left|class=skin-invert-image|Nalmexone synthesis

Excerpted from Wikipedia’s “nalmexone” article, available under the CC BY-SA 4.0 licence.

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