Potent melatonin receptor ligands
Novel compounds for modulation of MT1 and/or MT2 receptor activity
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Credit: State University of New York
State University of New York (SUNY) Chancellor John B. King Jr. today announced that this technology is a recipient of the latest round of seed funding through the SUNY Technology Accelerator Fund (TAF), which provides grants to faculty inventors and scientists.
Background:
Melatonin is an indoleamine hormone produced by the pineal gland. It is known primarily for its critical importance in regulating sleep promotion and circadian rhythms; however, melatonin has also been implicated in a broad range of unique functions. These include: regulation of blood pressure, inflammation and autoimmune conditions, e.g., inflammatory bowel disease (IBD) and rheumatoid arthritis (RA), pain sensing, memory formation and learning, neuroprotection in both stroke and neurodegenerative disorders, cancer, neuropsychiatric disorders such as depression, anxiety and addiction, and metabolic disorders such as diabetes and metabolic syndrome. The melatonin molecule acts through the MT1 and MT2 receptors, each of which is associated with different, often opposing effects. This has resulted in commercial interest in developing selective MT1 or MT2 receptor modulators. Despite this, no marketed therapies are currently available.
Technology Overview:
This University at Buffalo invention describes a series of side chain-substituted melatonin analogues and derivatives that are expected to act as novel agonists, partial agonists, inverse agonists, and/or antagonists with high affinity for the MT1 and/or MT2 receptors, including compounds expected to treat circadian rhythm disorders. This docket also includes MT2 selective partial agonists and antagonists that may counteract pain or have antidepressant-like activity.
Advantages:
- 120 novel compounds in two chemical categories
- Selective MT1/MT2 receptor binding demonstrated via radioligand binding assay
- Large and expanding global sleep therapeutics market (~$25B–$30B)
- In vivo phenotypic data available for some compounds
- Currently under active development for treatment of sleep disorders
Potential Applications:
- Circadian rhythm disorders
- Hypertension & stroke
- Psychiatric & pain disorders
- Inflammation & autoimmune conditions
- Metabolic disorders & diabetes
Intellectual Property Summary: Provisional patent application filed: US 63/912,281
Stage of Development: In vitro, TRL: 2 https://en.wikipedia.org/wiki/Technology_readiness_level
Licensing Status: Available for licensing or collaboration
Additional Information:
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