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Melatonin Discovery Leads to Promising Insomnia Drug


If you are plagued by insomnia, you may be somewhat reassured by a recent discovery about melatonin that explains the role of this “sleep hormone” in the brain. More importantly, the discovery led to the development of a drug that could open the door to new treatments for insomnia.

Melatonin holds a key to better sleep

Melatonin is a hormone produced by a tiny gland in the brain called the pineal gland. The primary role of melatonin is to help regulate sleep and wake cycles.

Melatonin production follows a cycle that is affected by light. Basically, melatonin levels rise in the mid to late evening hours, stay elevated most of the night, and then decline in the early morning hours. Levels of natural melatonin fall with age, leaving some older adults with little to no melatonin.

Investigators at the Research Institute of the McGill University Health Centre (RI-MUHC) and McGill University conducted research that uncovered the role of the melatonin receptors in the brain that promote deep sleep, receptors called MT2. Capitalizing on that discovery, they, along with a team of chemists from Parma, Italy, developed a new drug called UCM765, which can specifically activate MT2.

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This discovery is significant because until now, most treatments for insomnia, including benzodiazepines (e.g., Ativan, Halcion, Restoril, Valium), are not selective for deep sleep. Dr. Gabriella Gobbi, a researcher in psychiatry at the RI-MUHC and the study’s main investigator, explained why deep sleep is so important.

“Deep sleep has significant restorative effects, as well as the ability to increase memory and boost metabolism,” she noted, “while lowering blood pressure and slowing the heart rate.” Thus getting deep sleep not only can make you feel rested and energized, it is also critical for other important health factors.

The drug UCM765 was tested in rats and mice, where the researchers observed an increase in deep sleep in the animals. “The development of this pharmacology by means of targeting deep sleep receptors to treat insomnia represents a major advancement in our ability to deal with this common health problem that affects people worldwide,” noted Dr. Vassilios Papadopoulos, executive director and chief scientific officer of the RI-MUHC.

Insomnia is an inability to fall asleep or remain asleep, as well as waking up not feeling refreshed or restored. It can be acute, lasting one to several nights, or chronic, persisting for months to years. Insomnia is the most common sleep complaint among people in the United States.

The authors are hopeful their melatonin discovery and subsequent development of UCM765 will lead to the creation of new, effective treatments for insomnia. About 30 to 40% of adults report having symptoms of insomnia within a given year, and about 10 to 15% of adults say they have chronic insomnia, according to the National Center for Sleep Disorders Research.

McGill University Health Centre