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Nalmefene

Nalmefene structure

Nalmefene 

structure
  • CAS No:

    55096-26-9

  • Formula:

    C21H25NO3

  • Chemical Name:

    Nalmefene

  • Synonyms:

    [5ALPHA]-17-[CYCLOPROPYLMETHYL]-4,5-EPOXY-6-METHYLENEMORPHINAN-3,14-DIOL;17-(cyclopropylmethyl)-4,5alpha-epoxy-6-methylenemorphinan-3,14-diol;NALMEFENE;(5alpha)-17-(cyclopropylmethyl)-4,5-epoxy-6-methylenemorphinon-3,14-diol;6-desoxy-6-methylenenaltrexone;nalmetrene;(5α)-17-(cyclopropylmethyl)-4,5-epoxy-6-methylenemorphinan-3,14-diol;6-Deoxo-6-methylenenaltrexone

  • Categories:

    Pharmaceutical Intermediates  >  Bulk Drug Intermediates

Description

Nalmefene is a 6-methylene analogue of naltrexone. It is a pure opioid receptor antagonist and has a high affinity for the κ-opioid receptor. Nalmefene has a long duration of action and is used in oral and parenteral formulations.


Off-White Solid


ChEBI: Nalmefene is a morphinane alkaloid.


Nalmefene (Revex) is a pure opioid antagonist that is the6-methylene analog of naltrexone. It is available as a solutionfor IV, IM, or subcutaneous (SC) administration toreverse the effects of opioids after general anesthesia andin the treatment of overdose. It is longer acting than naloxonebut otherwise has a similar pharmacodynamic andmetabolic (3-glucuronidation) profile. Nalmefene hashigher oral bioavailability (approximately 40%) thannaloxone or naltrexone and is currently being investigatedas an oral treatment for pathological gambling and alcoholabuse.

Nalmefene Basic Attributes

339.44

339.43

White to Off-White

Characteristics

1.38±0.1 g/cm3(Predicted)

182-185C

507.9±50.0 °C(Predicted)

pKa 7.63(H2O) (Uncertain)

5.5×1010mol/(m3Pa) at 25℃, HSDB (2015)

2-8°C

Safety Information

3

Xi

26-36

36/37/38

Nalmefene Use and Manufacturing

A structural analog of Naltrexone (N285780) with opiate antagonist activity used in pharmaceutical treatment of alcoholism. Other pharmacological applications of this compound aim to reduce food cravings, drug abuse and pulmonary disease in affected individuals. Used as an opioid-induced tranquilizer on large animals in the veterinary industry. Narcotic antagonist.


A structural labelled analog of Naltrexone (N285780) with opiate antagonist activity used in pharmaceutical treatment of alcoholism. Other pharmacological applications of this compound aim to reduce f ood cravings, drug abuse and pulmonary disease in affected individuals. Used as an opioid-induced tranquilizer on large animals in the veterinary industry. Narcotic antagonist.


opioid antagonists therapeutic for alcohol dependence

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