CRF-1 Receptor Antagonists for PET Imaging or as Potential Therapeutics


Small molecule corticotrophin releasing factor 1 (CRF-1) antagonists, for use as PET imaging agents or potential therapeutics for treating generalized anxiety disorder.

Key Benefits

  • Can image CRF-1 receptor density and distribution via PET
  • Potential antagonist and therapeutics for psychological disorders including anxiety and depression

Technical Summary

Generalized anxiety disorder (GAD) is a common chronic disorder characterized by long-lasting anxiety that is not focused on any one object or situation. This excessive worry often interferes with daily life and functioning. It is estimated that in the US, approximately 9.5 million adults (3.1%) suffer from some variation of GAD, with a larger proportion of sufferers being female. The body’s stress system, particularly the stress hormone CRF-1 is believed to play a role in the disorder. CRF-1’s receptor has been acknowledged as a potential target for developing therapeutics to treat these disorders; however there are no currently available therapeutics directed toward the CRF-1 system, and few in development. This leaves the CRF system as an untapped resource for potential treatments.

Dr. Jeffrey Stehouwer and his colleagues have designed a group of small molecule compounds targeted to the CRF-1 receptor, initially for use as imaging agents during PET scanning. Some of the compounds within this group are also anticipated to work as receptor antagonists, binding to the receptor, but blocking or blunting the biological response. Beyond GAD, the CRF system and CRF-1 receptor are also believed to play a role in other psychological disorders such as depression, post-traumatic stress disorder (PTSD), and obsessive compulsive disorder (OCD) expanding the possible uses and markets for these compounds.

Developmental Stage

A small number of compounds have been generated. Proof of concept animal studies for PET imaging purposes are planned.

Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Nationalized PCT - United States United States 13/201,485 8,551,996 8/31/2011 10/8/2013 Issued
Tech ID: 09017
Published: 9/6/2011