Nalmefene

(5R, 9R, 13S, 14S ) -17 - cyclopropylmethyl -6-methylene -4 ,5- epoxymorphinan -3 ,14 -diol (IUPAC)

  • 55096-26-9
  • 58895-64-0 ( Nalmefenhydrochlorid )
  • 1228646-70-5 ( Nalmefenhydrochlorid · 2 H2O)

N07BB05

White solid (hydrochloride dihydrate )

Opioid antagonist

188-190 ° C

Attention

Template: Infobox chemical / molecular formula search is not available

Nalmefene is an opioid antagonist, which was developed in the 1970s. Previously been used as an antidote for treating Opiatvergiftungen, there is today in the treatment of alcoholism is used.

Field of application

Nalmefene was in March 2013 approved in the EU under the trade name Selincro for the reduction of alcohol consumption in adult patients with alcohol dependence, and alcohol consumption which is at a high level of risk and do not have physical withdrawal symptoms.

Mechanism of action

Nalmefene selectively binds to the opioid receptors. It has an antagonistic activity at the μ - and δ - receptors, partial agonist activity at the κ receptor.

Acute alcohol consumption leads to a release of dopamine in the mesolimbic system, which acts as a " positive reward system " and plays a role in the development of addiction. It is believed that nalmefene modulated cortico - mesolimbic functions, positive reinforcement oppressed us can thus reduce the consumption of alcohol.

CAS registry number Anatomical Therapeutic Chemical Classification System Dangerous Substances Directive (67/548/EEC) Receptor antagonist Mesolimbic pathway
591466
de