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  1. #1
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    A new therapeutic avenue for treating insomnia

    Insomnia is one of the major sleep problems with an estimated prevalence of 10% to 15% in the general population and 30% to 60% in the older population. Moreover, insomnia frequently co-occurs with a wide range of psychiatric disorders, including depression and anorexia. The most widely prescribed agents for the treatment of insomnia are benzodiazepines and non-benzodiazepines, which are central nervous system depressants that enhance signaling of the inhibitory neurotransmitter γ-aminobutyric acid. These medications, however, are plagued by a wide range of adverse effects, including muscle relaxation, rebound insomnia, changes in appetite, next-day sedation, cognitive impairment, amnesic effects, and development of drug tolerance and dependence. A new paper published on October 15, 2018 in the journal Neuropharmacology finds that enhancing endogenous signaling of adenosine A2A receptors may be an alternative strategy for treating insomnia.

    Adenosine has long been known to represent a state of relative energy deficiency and to induce sleep via adenosine receptors. Although adenosine A2A receptor agonists strongly induce sleep, their adverse cardiovascular effects preclude their use in treating sleep disorders. Researchers at the International Institute for Integrative Sleep Medicine (WPI-IIIS) at the University of Tsukuba succeeded in identifying the first positive allosteric modulator for adenosine A2A receptors and demonstrated that enhancing A2A receptor signaling induces sleep that is indistinguishable from the major component of natural sleep, known as slow-wave sleep, as it is characterized by slow and high-voltage brain waves, without affecting cardiovascular function. A positive allosteric modulator may evoke selective physiologic A2A receptor responses because, in contrast to an A2A receptor agonist, its actions are limited to when and where adenosine is released. "We believe that allosteric modulators of A2A receptors may help people with sleep problems to fall asleep" says Mustafa Korkutata, the first author of the paper.

    Although mice are the most commonly used model organism of human disease, results in mice, however, are often not always reliable for predicting human study outcomes. Therefore, "many obstacles remain to be overcome in generating a novel drug for the treatment of insomnia in humans, but we believe that our discovery will unlock the development of the next-generation sleeping pill." explained medicinal chemist Dr. Tsuyoshi Saitoh, another lead author of the paper.
    Once we accept our limits, we go beyond them. ~ Albert Einstein


  2. #2
    Power User johnes's Avatar
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    Useful info, tnx. Insomnia could be a serious disease, it's better to consult with specialist.

  3. #3
    Power User johnes's Avatar
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    That's true, I found benefits of weighted blanket therapy and it helped me to get rid of my insomnia in the short period of time, visit the website for more info.These blankets are quite comfortable, they are really good stuff. After a few nights you will notice that your sleep pattern has improved
    Last edited by johnes; 05-15-2020 at 09:33 AM.

  4. #4
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    I have suffered from it since i can remember my eyes start to burn because of the lack of rest and only taking methocarbamol and amitriptyline 50mg (most times 3/4 of each) can make me sleep and now with the lockdown its even worse unfortunately its life

    Everyone please be safe

  5. #5
    Power User nickolelee's Avatar
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    Good sleep often defines the quality of life in general, especially it's psychological aspect. I coped with my sleep disorder due to long-lasting therapy and medical support, I also used my cbd oil cartridge vaporizer regularly, with a Smart Cart battery.


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