Belsomra
From Proteopedia
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- | <scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref>DOI: 10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep | + | <scene name='74/746099/Belsomra/1'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat the inability to fall asleep or stay asleep <ref name="one">DOI: 10.1097/01.NAJ.0000457406.61092.35</ref>. While most other insomnia drugs, like Ambien and Lunesta, are GABA agonists and work to slow down neuronal firings, Belsomra is the first drug to target orexin <ref>doi: 10.1017/S1092852916000225</ref>. Orexin, also known as hypocretin, is a neurotransmitter that binds to receptors in order to cause alertness and wakefulness. By targeting these neurotransmitters, it cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />. |
== Function == | == Function == | ||
The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1). | The orexin neuropeptides, Orexin-A and Orexin-B, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems (4). These orexin neuropeptides bind to the receptors, Orexin receptors types 1 and 2, which are G protein coupled receptors (GPCRs). The GPCRs can sense a molecule outside the cell and send a signal through transduction in order to cause the cells to respond (5). Thus, binding of the two can control wakefulness and sleep in homo sapiens. In studies, Orexin-B has shown to be more selective in binding, choosing to bind to Orexin receptor type 2 a majority of the time. Orexin-A has shown an equal selectivity at both types of receptors (4). Belsomra is a dual orexin receptor antagonist, and has the ability to block both Orexin receptors 1 and 2, thus inhibiting the neuropeptides from binding. By blocking this interaction, sleep can occur (1). |
Revision as of 18:13, 28 November 2016
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References
- ↑ Hanson, R. M., Prilusky, J., Renjian, Z., Nakane, T. and Sussman, J. L. (2013), JSmol and the Next-Generation Web-Based Representation of 3D Molecular Structure as Applied to Proteopedia. Isr. J. Chem., 53:207-216. doi:http://dx.doi.org/10.1002/ijch.201300024
- ↑ Herraez A. Biomolecules in the computer: Jmol to the rescue. Biochem Mol Biol Educ. 2006 Jul;34(4):255-61. doi: 10.1002/bmb.2006.494034042644. PMID:21638687 doi:10.1002/bmb.2006.494034042644
- ↑ 3.0 3.1 doi: https://dx.doi.org/10.1097/01.NAJ.0000457406.61092.35
- ↑ Stahl SM. Mechanism of action of suvorexant. CNS Spectr. 2016 Jun;21(3):215-8. doi: 10.1017/S1092852916000225. PMID:27322687 doi:http://dx.doi.org/10.1017/S1092852916000225
First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 114(12):26, December 2014.
Krystal AD, Benca RM, Kilduff TS. Understanding the sleep-wake cycle: sleep, insomnia, and the orexin system. J Clin Psychiatry 2013; 74(Suppl 1): 3–20.
Pagel, J. F., & Parnes, B. L. (2001). Medications for the Treatment of Sleep Disorders: An Overview. Primary Care Companion to The Journal of Clinical Psychiatry, 3(3), 118–125.
Schwartz, J. R. ., & Roth, T. (2008). Neurophysiology of Sleep and Wakefulness: Basic Science and Clinical Implications. Current Neuropharmacology, 6(4), 367–378. http://doi.org/10.2174/157015908787386050
Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225.
Sutton, E. L. (2015). Profile of suvorexant in the management of insomnia. Drug Design, Development and Therapy, 9, 6035–6042. http://doi.org/10.2147/DDDT.S73224
T. Sakurai, A. Amemiya, M. Ishii, I. Matsuzaki, R.M. Chemelli, H. Tanaka, S.C. Williams, J.A. Richardson, G.P. Kozlowski, S. Wilson, J.R. Arch, R.E. Buckingham, A.C. Haynes, S.A. Carr, R.S. Annan, D.E. McNulty, W.S. Liu, J.A. Terrett, N.A. Elshourbagy, D.J. Bergsma, M. Yanagisawa Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell, 92 (1998), pp. 573–585.
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