Modulated interaction of μ/δ opioid receptors and the drug discovery and design strategy
- VernacularTitle:μ/δ阿片受体相互调节作用及药物发现与设计策略
- Author:
Qing SHEN
;
Huifang LIU
;
Wei LI
;
Ying LI
;
Jiagao CHENG
;
Jinggen LIU
;
Wei FU
- Publication Type:Journal Article
- Keywords:
μ/δ agonist;
μ agonist/δ antagonist;
opioid analgesics;
drug design;
low addiction;
dual action
- From:
Chinese Pharmacological Bulletin
2010;26(1):4-8
- CountryChina
- Language:Chinese
-
Abstract:
Opioid analgesics are potent pain-killer and are widely used in clinical practice.Opioid receptors are classified into μ,δ,κ subtypes.Most of the currently available opioid analgesics are μ opioid receptor agonists, but they cause undesired side effects such as physical dependence, respiratory depression and constipation and so on.The antalgic activity of δ receptor agonist is weaker than that of μ agonist, but it can modulate the activity of μ receptor and prevent its addiction. Therefore, discovering and designing compounds with μ/δ dual action is a new way for finding analgesics with low toxicity and less side effects.This review summarizes the development of compound with dual μ/δ activities and provides a new strategy for designing analgesics with low toxicity and less side effects.
