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PAC1R Inhibitors for Treatment of Pain and Stress Related Disorders | UVM Innovations | University of Vermont

PAC1R Inhibitors for Treatment of Pain and Stress Related Disorders

UVM Reference Number: C759

Summary:

PACAP signaling has been identified in multiple intersecting stress and pain associated pathologies

Background:

The healthcare and loss of productivity costs of pain and stress related disorders now exceed those of cardiovascular disease, cancer and diabetes. More than 65 million adults are affected by anxiety disorders in the United States and Europe alone and healthcare costs in the US exceed $42 billion a year. There are currently few therapeutic options to address this problem and what is available often fails to offer relief or produces undesirable side effects.

Technology Overview:

Pituitary adenylate cyclase-activating polypeptide (PACAP) signaling has been identified in multiple intersecting stress and pain associated pathologies, including PTSD, migraine, neuropathic and emotional pain and panic disorders. More specifically, antagonists that preferentially block the internalization and endosomal signaling of the G-protein coupled receptor (GPCR) pituitary adenylate cyclase-activating polypeptide receptor (PAC1R) have been shown to have high efficacy in attenuating these behavioral and pain disorders, but until now, no have been developed. GPCR structure-based drug design in one University of Vermont laboratory has identified several lead compounds, which show the necessary efficacy to have therapeutic potential in the researchers' assays and in vivo stress/anxiety tests. The research team are currently modifying these leads to increase potency and specificity.