Belsomra
From Proteopedia
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<StructureSection load='4S0V' size='340' side='right' caption=scene=''> | <StructureSection load='4S0V' size='340' side='right' caption=scene=''> | ||
- | Belsomra, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: http://dx.doi.org/10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are Gamma-aminobutyric acid (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, Belsomra cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />. | + | <scene name='74/746099/Belsomra/4'>Belsomra</scene>, also known as Suvorexant, is a medication used to treat insomnia. <ref name="one">Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: http://dx.doi.org/10.1097/01.NAJ.0000457406.61092.35. </ref>. While most other insomnia drugs, like Ambien and Lunesta, are Gamma-aminobutyric acid (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, Belsomra cuts off the signals causing one to be awake, and will result in sleep <ref name="one" />. |
== Function == | == Function == | ||
The orexin neuropeptides, <scene name='74/746099/Orexin-a/1'>Orexin-A</scene> and <scene name='74/746099/Orexin-b/1'>Orexin-B</scene>, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. 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 <ref>PMID:9491897 </ref>. 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 <ref name="two" />. 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 <ref name="one" />. | The orexin neuropeptides, <scene name='74/746099/Orexin-a/1'>Orexin-A</scene> and <scene name='74/746099/Orexin-b/1'>Orexin-B</scene>, can excite neurons in the brain and affect multiple systems, including the acetylcholine, dopamine, histamine, and norepinephrine systems <ref name="two">doi:10.4088/JCP.13011su1c </ref>. 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 <ref>PMID:9491897 </ref>. 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 <ref name="two" />. 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 <ref name="one" />. |
Revision as of 21:05, 6 December 2016
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References
- ↑ 1.0 1.1 1.2 Aschenbrenner, DS. First Orexin Receptor Antagonist Approved for Insomnia. AJN, American Journal of Nursing. 2014 Dec;114(12):26. doi: http://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
- ↑ 3.0 3.1 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. doi: 10.4088/JCP.13011su1c. PMID:24107804 doi:http://dx.doi.org/10.4088/JCP.13011su1c
- ↑ Sakurai T, Amemiya A, Ishii M, Matsuzaki I, Chemelli RM, Tanaka H, Williams SC, Richardson JA, Kozlowski GP, Wilson S, Arch JR, Buckingham RE, Haynes AC, Carr SA, Annan RS, McNulty DE, Liu WS, Terrett JA, Elshourbagy NA, Bergsma DJ, Yanagisawa M. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998 Feb 20;92(4):573-85. PMID:9491897
- ↑ Yin J, Mobarec JC, Kolb P, Rosenbaum DM. Crystal structure of the human OX orexin receptor bound to the insomnia drug suvorexant. Nature. 2014 Dec 22. doi: 10.1038/nature14035. PMID:25533960 doi:http://dx.doi.org/10.1038/nature14035
- ↑ Yin J, Mobarec JC, Kolb P, Rosenbaum DM. Crystal structure of the human OX orexin receptor bound to the insomnia drug suvorexant. Nature. 2014 Dec 22. doi: 10.1038/nature14035. PMID:25533960 doi:http://dx.doi.org/10.1038/nature14035
- ↑ Yin J, Mobarec JC, Kolb P, Rosenbaum DM. Crystal structure of the human OX orexin receptor bound to the insomnia drug suvorexant. Nature. 2014 Dec 22. doi: 10.1038/nature14035. PMID:25533960 doi:http://dx.doi.org/10.1038/nature14035
- ↑ Yin J, Mobarec JC, Kolb P, Rosenbaum DM. Crystal structure of the human OX orexin receptor bound to the insomnia drug suvorexant. Nature. 2014 Dec 22. doi: 10.1038/nature14035. PMID:25533960 doi:http://dx.doi.org/10.1038/nature14035
- ↑ 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. doi: http://dx.doi.org/10.4088/PCC.v03n0303
- ↑ Schwartz JR, Roth T. Neurophysiology of sleep and wakefulness: basic science and clinical implications. Curr Neuropharmacol. 2008 Dec;6(4):367-78. doi: 10.2174/157015908787386050. PMID:19587857 doi:http://dx.doi.org/10.2174/157015908787386050
- ↑ Sutton EL. Profile of suvorexant in the management of insomnia. Drug Des Devel Ther. 2015 Nov 11;9:6035-42. doi: 10.2147/DDDT.S73224. eCollection, 2015. PMID:26648692 doi:http://dx.doi.org/10.2147/DDDT.S73224
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