Novel Opioid Receptor Agonists with Reduced Morphine-like Side Effects

Title:Novel Opioid Receptor Agonists with Reduced Morphine-like Side Effects

Volume: 18 Issue: 19

Author(s): Lianghan Zhu, Zhiying Cui, Qihua Zhu, Xiaoming Zha and Yungen Xu*

Affiliation:

• Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009,China

Keywords: Opioid receptor agonists, morphine-like side effects, β-arrestin2 recruitment, allosteric modulators, MOR, GPCR.

Abstract: Opioid analgesics, such as morphine, are widely employed in the treatment of moderate to severe pain. However, they are notorious for abuse liability and respiratory depression. Therefore circumventing the side effects, such as euphoria, addiction, respiratory depression and gastrointestinal adverse reactions, is of extensive importance. Recently, a large number of research results have revealed that such morphine-like side effects are not inevitable, and they focus on the novel approaches to disconnecting the analgesics from adverse effects. In this review, we mainly discuss the approaches including biasing the GPCRs over β-arrestin2 recruitment (TRV130, PZM21, HS665), the positive allosteric modulators of the MOR (BMS-986122) and multiple agonists of opioid receptors subtypes (SNC80, DPI-125). Besides these, we also introduce the key protein sites of MOR and β-arrestin2 recruitment briefly.

Cite this article as:

Zhu Lianghan , Cui Zhiying , Zhu Qihua , Zha Xiaoming and Xu Yungen *, Novel Opioid Receptor Agonists with Reduced Morphine-like Side Effects, Mini-Reviews in Medicinal Chemistry 2018; 18 (19) . https://dx.doi.org/10.2174/1389557518666180716124336