类阿片
羟考酮
药理学
变构调节
受体
慢性疼痛
吗啡
阿片受体
止痛药
变构调节剂
医学
内科学
精神科
作者
Kristin L. Rockwell,Andrew Alt
出处
期刊:The Royal Society of Chemistry eBooks
[The Royal Society of Chemistry]
日期:2016-11-18
卷期号:: 194-219
标识
DOI:10.1039/9781782629276-00194
摘要
Activation of opioid receptors produces powerful analgesia; and µ-opioid receptor agonists such as morphine and oxycodone remain the “gold standard” for pain therapy, despite their abuse liability and dangerous side effect profile. Safer pain medications are urgently needed. The recent discovery of positive allosteric modulators (PAMs) of µ- and δ-opioid receptors provides a new approach for exploiting the analgesic effects of opioid receptor activation. PAMs enhance endogenous opioid signaling but do not activate the receptor directly, and therefore may be expected to exert analgesic effects while improving upon the side effect profile and abuse liability associated with direct-acting opioid agonists. The discovery and characterization of the first opioid PAM molecules is described, as well as the rationale for the development of opioid PAMs as novel therapeutic agents for the treatment of pain.
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