Small molecule corticotropin-releasing factor antagonists

Abstract

Corticotropin-releasing factor (CRF) is a 41-amino acid peptide neurohormone that plays a major role in the body’s response to stress by modulating the endocrine, autonomic, behavioural and immune systems. The peptide interacts with two known receptors, CRF₁ and CRF₂, which belong to class B (secretin-like) G-protein-coupled receptors. Over the past ten years, a number of small molecule antagonists have been published in the patent literature. The present review covers recent patent literature (since 2000) where low molecular weight, non-peptide CRF antagonists are disclosed. These can be divided into four main classes of molecules: monocyclic, bicyclic and tricyclic compounds as well as a miscellaneous category, which include compounds that are unlike the traditional small molecule CRF₁ antagonists.

• antagonist
• anxiety
• corticotropin-releasing factor (CRF)
• depression
• stress