Antagonists of the kappa opioid receptor

作者：Urbano Mariangela; Guerrero Miguel; Rosen Hugh; Roberts Edward^*

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(9): 2021-2032.

DOI：10.1016/j.bmcl.2014.03.040

• OPRK antagonists
• Short-acting
• Depression
• Addictive disorders
• Stress-related disorders

The research community has increasingly focused on the development of OPRK antagonists as pharmacotherapies for the treatment of depression, anxiety, addictive disorders and other psychiatric conditions produced or exacerbated by stress. Short-acting OPRK antagonists have been recently developed as a potential improvement over long-acting prototypic ligands including nor-BNI and JDTic. Remarkably the short-acting LY2456302 is undergoing phase II clinical trials for the augmentation of the antidepressant therapy in treatment-resistant depression. This Letter reviews relevant chemical and pharmacological advances in the identification and development of OPRK antagonists.

• 出版日期2014-5-1