Basal opioid receptor activity, neutral antagonists, and therapeutic opportunities
作者： Wolfgang Sadée , Danxin Wang , Edward J. Bilsky
DOI: 10.1016/J.LFS.2004.10.024
关键词:
摘要: Abstract The μ opioid receptor (MOR, OPRM) – the principal involved in narcotic addiction– has been shown to display basal (spontaneous, constitutive) signaling activity. Interaction with other proteins, such as calmodulin, regulates MOR Providing a mechanism for long-lasting regulation, activity potentially plays key role addiction, combination gene regulation and synaptic remodeling. Recent results support link physical dependence one of main manifestations addiction drugs abuse. prototypical antagonists, naloxone naltrexone, were act inverse agonists morphine-dependent state (i.e., they suppress signaling) thereby appear elicit or contribute precipitated withdrawal. This affords opportunity explore therapeutic applications neutral antagonists (blocking at without affecting activity) reduced adverse effects. Neutral are promising drug candidates treatment overdose, peripheral effects analgesics.
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