Belsomra: Difference between revisions
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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). | ||
== Structural | == Structural Highlights == | ||
==Relationship to Insomnia== | ==Relationship to Insomnia== | ||
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Stahl, S.M. (2016) ‘Mechanism of action of suvorexant’, CNS Spectrums, 21(3), pp. 215–218. doi: 10.1017/S1092852916000225. | 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. | 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. | ||
