Hydrolysis-Resistant Local Anesthetics
OHSU # 1684
CNG CHANNEL BLOCKERS
FOR TREATMENT OF RETINAL DISEASE
OHSU Technology 1684
To meet a pressing need for better cyclic nucleotide-gated (CNG) channel antagonists, Researchers at Oregon Health & Science University and Willamette University designed, synthesized and determined the apparent affinities and mechanism of CNG channel block with novel hydrolysis resistant tetracaine derivatives. Alterations of CNG channel activity are central in the pathology of certain forms of retinal degeneration including some forms of retinitis pigmentosa. Therefore, these compounds may meet an unmet medical need for therapeutic agents that treat retinal disease.
Retinitis pigmentosa (RP) refers to a group of inherited diseases causing retinal degeneration. The cell-rich retina lines the back inside wall of the eye. It is responsible for capturing images from the visual field. People with RP experience a gradual decline in their vision because photoreceptor cells (rods and cones) die. CNG ion channels are known for their role in phototransduction in retinal photoreceptors and in odorant transduction in the olfactory epithelium. CNG channel activation in photoreceptors is regulated by the cytoplasmic concentration of cGMP, which binds to and opens the channel to allow influx of Na+ and Ca2+ ions. CNG channel blockers can therefore be effective treatments for these blinding diseases.
· 100,000 people in USA suffer from retinitis pigmentosa
· Nutritional therapy with Vitamin A, and Docosahexaenoic Acid
· Gene therapies and therapeutic agents are under preclinical and clinical evaluation
While at OHSU, Dr. Jeffrey W. Karpen focused on the fundamental mechanisms of cellular signaling with an emphasis on signaling by the intracellular messengers cAMP and cGMP.
US Provisional patent application filed 12/16/2011
US Non-provisional patent application filed 12/14/2012 and published as US2014/0018422
OHSU Technology 1684 is available for exclusive licensing and collaborative co-development.
Karpen JW et al. J Med Chem. 2011, 54(13):4904-12.
Karpen JW et al. Bioorg Med Chem Lett. 2011, 21(21):6417-9.
- Jeffrey Karpen
- Sarah Kirk
- Adriana Andrade, SM.Physiology & Pharmacology
- Kenneth Melich, SM.Physiology & Pharmacology
- Michelle Schaffer
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