The neuroimmunopharmacology of opioids and the CNS drug discovery  

出　　处：《中国药理学通报》2015年第B11期57-57,共1页Chinese Pharmacological Bulletin

摘　　要：Opioids have been used for treated pain for thousands of years. Meanwhile, opioids induce drug addic- tion, which causes serious medical and social problems. Most opioids research have been concentrated on neurons in the central nerve system （CNS） , however, the action of glia, which accounts for 90% cells in CNS have been long neglected. Unlike the classical opioid-neuron stereoselective interaction opioids were found to non-stereose- lectively bind the accessory protein myeloid differentiation factor 2 （MD-2） of innate immune Toll- like receptor 4 （TLR4） , which induces glial activation and pro-inflammatory factors production, therefore contributing to opioid hyper-analgesia, drug tolerance, dependence and addiction. A series of TLR4 antagonists have been discovered by multiple drug discovery strategies for inhibiting the opioids＇ side effects and treating drug abuse, among which （ ＋ ）-naltrexone and T-5342126 have been transferred to Xalud and BioLineRx respectively, for further pre-clini- cal/clinical drug development.

关 键 词：TLR4 MD2 OPIOID INNATE immune GLIA DRUG dependence DRUG ADDICTION 

分 类 号：R[医药卫生]