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Bioorg Med Chem Lett. 2014 May 1;24(9):2021-32. doi: 10.1016/j.bmcl.2014.03.040. Epub 2014 Mar 24.

Antagonists of the kappa opioid receptor.

Author information

1
Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States.
2
Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States; The Scripps Research Institute Molecular Screening Center, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States; Department of Immunology, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States.
3
Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, United States. Electronic address: eroberts@scripps.edu.

Abstract

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.

KEYWORDS:

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

PMID:
24690494
DOI:
10.1016/j.bmcl.2014.03.040
[Indexed for MEDLINE]

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