Research progress of novel opioid analgesics
- VernacularTitle:新型阿片类镇痛药的研发进展
- Author:
Chunbo HE
1
,
2
;
Dan WANG
2
,
3
;
Shujia YANG
2
,
3
;
Kaiwen ZHOU
2
,
3
;
Yiping DENG
1
,
2
;
Shouliang DONG
4
Author Information
1. School of Pharmacy，Dezhou University，Shandong Dezhou 253023，China
2. Shandong Engineering Research Center of Novel Pharmaceutical Excipients，Sustained and Controlled Release Preparations，Shandong Dezhou 253023，China
3. Medical School of Health，Dezhou University，Shandong Dezhou 253023，China
4. Dept. of Animal and Biomedical Sciences，School of Life Sciences，Lanzhou University，Lanzhou 730000，China
- Publication Type:Journal Article
- Keywords:
opioid analgesic;
biased agonist;
one drug-multiple targets;
peripheral agonist;
new drug development
- From:
China Pharmacy
2024;35(17):2176-2180
- CountryChina
- Language:Chinese
-
Abstract:
Opioid analgesics are currently known as the best analgesics. However， toxicity and side effects such as constipation， tolerance and addiction severely limit their clinical application. With the in-depth understanding of the signal transduction mechanism of opioid receptors and the continuous advancement of drug design technology， researchers have managed to develop many promising new methods to get low-toxic and more efficient opioid analgesics， which are different from the traditional morphine skeleton structure modifications. This article focuses on three new research strategies of G-protein biased activation，“ one drug-multiple targets” and peripheral activation. The basic principles of relative separation of analgesic activity and adverse drug reaction by each strategy are introduced， and the latest research progress of representative drugs is briefly reviewed. Among them， the recently approved novel opioid analgesics oliceridine and tegileridine are G-protein biased μ-opioid receptor agonists， Cebranopadol is a typical “one drug-multiple targets” analgesic， and NFEPP is a representative drug of peripheral opioid receptor agonists. The above several strategies complement each other and provide reference for the development of new opioid analgesic drugs.
