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Discovery And Development Of Melatonin Receptor Agonists
Melatonin receptor agonists are analogues of melatonin that bind to and activate the melatonin receptor. Agonists of the melatonin receptor have a number of therapeutic applications including treatment of sleep disorders and depression. The discovery and development of melatonin receptor agonists was motivated by the need for more potent analogues than melatonin, with better pharmacokinetics and longer half-lives. Melatonin receptor agonists were developed with the melatonin structure as a model. The melatonin receptors are G protein-coupled receptors and are expressed in various tissues of the body. There are two subtypes of the receptor in humans, melatonin receptor 1 (MT1) and melatonin receptor 2 (MT2). Melatonin and melatonin receptor agonists, on market or in clinical trials, all bind to and activate both receptor types. The binding of the agonists to the receptors has been investigated since 1986, yet is still not fully understood. When melatonin receptor agonists bind t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melatonin Receptor
Melatonin receptors are G protein-coupled receptors (GPCR) which bind melatonin. Three types of melatonin receptors have been cloned. The MT1 (or Mel1A or MTNR1A) and MT2 (or Mel1B or MTNR1B) receptor subtypes are present in humans and other mammals, while an additional melatonin receptor subtype MT3 (or Mel1C or MTNR1C) has been identified in amphibia and birds. The receptors are crucial in the signal cascade of melatonin. In the field of chronobiology, melatonin has been found to be a key player in the synchrony of biological clocks. Melatonin secretion by the pineal gland has circadian rhythmicity regulated by the suprachiasmatic nucleus (SCN) found in the brain. The SCN functions as the timing regulator for melatonin; melatonin then follows a feedback loop to decrease SCN neuronal firing. The receptors MT1 and MT2 control this process. Melatonin receptors are found throughout the body in places such as the brain, the retina of the eye, the cardiovascular system, the liv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Xenopus Laevis
The African clawed frog (''Xenopus laevis''), also known as simply xenopus, African clawed toad, African claw-toed frog or the ''platanna'') is a species of African aquatic frog of the family Pipidae. Its name is derived from the short black claws on its feet. The word ''Xenopus'' means 'strange foot' and ''laevis'' means 'smooth'. The species is found throughout much of Sub-Saharan Africa (Nigeria and Sudan to South Africa), and in isolated, introduced populations in North America, South America, Europe, and Asia. All species of the family Pipidae are tongueless, toothless and completely aquatic. They use their hands to shove food in their mouths and down their throats and a hyobranchial pump to draw or suck things in their mouth. Pipidae have powerful legs for swimming and lunging after food. They also use the claws on their feet to tear pieces of large food. They have no external eardrums, but instead subcutaneous cartilaginous disks that serve the same function. They use ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MT1 Melatonin Receptor Signaling
{{Letter-NumberCombDisambig ...
MT-1, MT-01, MT1 or MT 1 may refer to: * MT 1, Montana Highway 1 * MT-1, Montana's 1st congressional district * Yamaha MT-01, a motorcycle * MT-1 airplane, see Manshū Hayabusa * MT1 protein, see Melatonin receptor 1A Melatonin receptor type 1A is a protein that in humans is encoded by the ''MTNR1A'' gene. Function This gene encodes the MT1 protein, one of two high-affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Non-24-hour Sleep–wake Disorder
Non-24-hour sleep–wake disorder (non-24, N24SWD, or N24) is one of several chronic circadian rhythm sleep disorders (CRSDs). It is defined as a "chronic steady pattern comprising ..daily delays in sleep onset and wake times in an individual living in a society". Symptoms result when the non-entrained ( free-running) endogenous circadian rhythm drifts out of alignment with the light–dark cycle in nature. Although this sleep disorder is more common in blind people, affecting up to 70% of the totally blind, it can also affect sighted people. Non-24 may also be comorbid with bipolar disorder, depression, and traumatic brain injury. The American Academy of Sleep Medicine (AASM) has provided CRSD guidelines since 2007 with the latest update released in 2015. People with non-24 experience daily shifts in the circadian rhythm such as peak time of alertness, body temperature minimum, metabolism and hormone secretion. These shifts do not align with the natural light–dark cycle. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orphan Drug
An orphan drug is a medication, pharmaceutical agent that is developed to treat certain rare medical conditions. An orphan drug would not be profitable to produce without government assistance, due to the small population of patients affected by the conditions. The conditions that orphan drugs are used to treat are referred to as orphan diseases. The assignment of orphan status to a disease and to drugs developed to treat it is a matter of public policy that depends on the legislation (if there is any) of the country. Designation of a drug as an orphan drug has yielded medical breakthroughs that might not otherwise have been achieved, due to the economics of drug medical research, research and development. Examples of this can be that in the U.S. and the EU, it is easier to gain marketing approval for an orphan drug. There may be other financial incentives, such as an extended period of exclusivity, during which the producer has sole rights to market the drug. All are intended to en ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Food And Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, Prescription drug, prescription and Over-the-counter drug, over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, Animal feed, animal foods & feed and Veterinary medicine, veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C). However, the agency also enforces other laws, notably Section 361 of the Public Health Service Act as well as associated regulations. Much of this regulatory-enforcement work is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tasimelteon
Tasimelteon, sold under the brand name Hetlioz, is a medication approved by the U.S. Food and Drug Administration (FDA) in January 2014, for the treatment of non-24-hour sleep–wake disorder (also called non-24, N24 and N24HSWD). In June 2014, the European Medicines Agency (EMA) accepted an EU filing application for tasimelteon and in July 2015, the drug was approved in the European Union for the treatment of non-24-hour sleep-wake rhythm disorder in totally blind adults, but not in the case of non-24 in sighted people. The most common side effects include headache, somnolence, nausea (feeling sick) and dizziness. Medical uses In the United States, tasimelteon capsules are indicated for the treatment of non-24-hour sleep–wake disorder (Non-24) in adults and for the treatment of nighttime sleep disturbances in Smith-Magenis Syndrome (SMS) in people sixteen years of age and older. Tasimelteon oral suspension is indicated for the treatment of nighttime sleep disturbances in S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Major Depressive Disorder
Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive depression (mood), low mood, low self-esteem, and anhedonia, loss of interest or pleasure in normally enjoyable activities. Introduced by a group of US clinicians in the mid-1970s, the term was adopted by the American Psychiatric Association for this syndrome, symptom cluster under mood disorders in the 1980 version of the ''Diagnostic and Statistical Manual of Mental Disorders'' (DSM-III), and has become widely used since. The disorder causes the second-most years lived with disability, after low back pain, lower back pain. The diagnosis of major depressive disorder is based on the person's reported experiences, behavior reported by family or friends, and a mental status examination. There is no laboratory test for the disorder, but testing may be done to rule out physical conditions that can cause similar symptoms. The most common time o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agomelatine
Agomelatine, sold under the brand names Valdoxan and Thymanax, among others, is an atypical antidepressant most commonly used to treat major depressive disorder and generalized anxiety disorder. One review found that it is as effective as other antidepressants with similar discontinuation rates overall but fewer discontinuations due to side effects. Another review also found it was similarly effective to many other antidepressants. Common side effects include headaches, nausea, and dizziness, which usually subside in the first few weeks, as well as liver problems – due to the potential effect on the liver, blood tests before treatment initiation, at specific time-points after initiation, and after dose increase is recommended. Its use is not recommended in people with dementia, or who are under the age of 18 or over 75. There is tentative evidence that it may have fewer side effects than some other antidepressants. It acts by serotonin receptor antagonist, blocking certain ser ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Circadin
Melatonin is a naturally occurring hormone produced in the brain that is also used as a dietary supplement and medication. As a hormone, melatonin is released by the pineal gland and is involved in sleep–wake cycles. As a supplement, it is often used for the short-term treatment of disrupted sleep patterns such as from jet lag or shift work, and is typically taken orally. There is evidence of its benefit for insomnia, but the evidence is not strong. A 2017 review found that sleep onset occurred six minutes faster with use on average, but found no change in total time asleep. Side effects from melatonin supplements are minimal at low doses for short durations (the studies reported that side effects occurred about equally for both melatonin and placebo). Side effects of melatonin are rare but may occur in 1 to 10 patients out of 1,000. They may include somnolence, headaches, nausea, diarrhea, abnormal dreams, irritability, restlessness, insomnia, anxiety, migraine, lethargy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Insomnia
Insomnia, also known as sleeplessness, is a sleep disorder where people have difficulty sleeping. They may have difficulty falling asleep, or staying asleep for as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, irritability, and a depression (mood), depressed mood. It may result in an increased risk of accidents of all kinds as well as problems focusing and learning. Insomnia can be short term, lasting for days or weeks, or long term, lasting more than a month. The concept of the word ''insomnia'' has two distinct possibilities: insomnia disorder (ID) or insomnia symptoms, and many abstracts of randomized controlled trials and systematic reviews often underreport on which of these two possibilities the word refers to. Insomnia can occur independently or as a result of another problem. Conditions that can result in insomnia include psychological stress, chronic pain, heart failure, hyperthyroidism, heartburn, restless leg syndrome, menopause ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ramelteon
Ramelteon, sold under the brand name Rozerem among others, is a melatonin agonist medication which is used in the treatment of insomnia. It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset. It reduces the time taken to fall asleep, but the degree of clinical benefit is small. The medication is approved for long-term use. Ramelteon is taken oral administration, by mouth. Side effects of ramelteon include somnolence, dizziness, fatigue (medical), fatigue, nausea, exacerbated insomnia, and changes in hormone levels. Ramelteon is an structural analog, analogue of melatonin (medication), melatonin and is a binding selectivity, selective agonist of the melatonin receptor, melatonin MT1 receptor, MT1 and MT2 receptor, MT2 receptors. The elimination half-life, half-life and duration of action, duration of ramelteon are much longer than those of melatonin. Ramelteon is not a benzodiazepine or Z-drug and does not interact with GABA r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
