Effects of a newly developed potent orexin-2 receptor-selective antagonist, compound 1 m, on sleep/wakefulness states in mice

Frontiers in Neuroscience

Volumn , Issue 8 JAN, 2014, Pages

  Etori, Keishi ^a   Saito, Yuki C ^a   Tsujino, Natsuko ^a   Sakurai, Takeshi ^a  

^a KANAZAWA UNIVERSITY   (Japan)

Author keywords

Orexin; Orexin receptor antagonists; REM sleep; Sleep; Wakefulness

Indexed keywords

C 1M; CHEMICALS AND DRUGS; OREXIN 2 RECEPTOR; SELECTIVE OREXIN 2 RECEPTOR ANTAGONIST; SUVOREXANT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; LOCUS CERULEUS; MONOAMINE NERVE CELL; MOUSE; NONHUMAN; NONREM SLEEP; NORADRENERGIC NERVE; REM SLEEP; SEROTONINERGIC NERVE CELL; SLEEP TIME; SLEEP WAKING CYCLE; WAKEFULNESS;

EID: 84898027536     PISSN: 16624548     EISSN: 1662453X     Source Type: Journal    
DOI: 10.3389/fnins.2014.00008     Document Type: Article

References (27)

1. Brisbare-Roch, C., Dingemanse, J., Koberstein, R., Hoever, P., Aissaoui, H., Flores, S., et al. (2007). Promotion of sleep by targeting the orexin system in rats, dogs and humans. Nat. Med. 13, 150-155. doi: 10.1038/nm1544.
2. Carter, M. E., Adamantidis, A., Ohtsu, H., Deisseroth, K., and De Lecea, L. (2009). Sleep homeostasis modulates hypocretin-mediated sleep-to-wake transitions. J. Neurosci. 29, 10939-10949. doi: 10.1523/JNEUROSCI.1205-09.2009.
3. Chemelli, R. M., Willie, J. T., Sinton, C. M., Elmquist, J. K., Scammell, T., Lee, C., et al. (1999). Narcolepsy in orexin knockout mice: molecular genetics of sleep regulation. Cell 98, 437-451. doi: 10.1016/S0092-8674(00)81973-X.
4. Cox, C. D., Breslin, M. J., Whitman, D. B., Schreier, J. D., Mcgaughey, G. B., Bogusky, M. J., et al. (2010). Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. J. Med. Chem. 53, 5320-5332. doi: 10.1021/jm100541c.
5. Dietrich, H., and Jenck, F. (2010). Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant. Psychopharmacology (Berl) 212, 145-154. doi: 10.1007/s00213-010-1933-5.
6. Dugovic, C., Shelton, J. E., Aluisio, L. E., Fraser, I. C., Jiang, X., Sutton, S. W., et al. (2009). Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J. Pharmacol. Exp. Ther. 330, 142-151. doi: 10.1124/jpet.109.152009.
7. Fujimoto, T., Kunitomo, J., Tomata, Y., Nishiyama, K., Nakashima, M., Hirozane, M., et al. (2011). Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists. Bioorg. Med. Chem. Lett. 21, 6414-6416. doi: 10.1016/j.bmcl.2011.08.093.
8. Hara, J., Beuckmann, C. T., Nambu, T., Willie, J. T., Chemelli, R. M., Sinton, C. M., et al. (2001). Genetic ablation of orexin neurons in mice results in narcolepsy, hypophagia, and obesity. Neuron 30, 345-354. doi: 10.1016/S0896-6273(01)00293-8.
9. Hoever, P., De Haas, S., Winkler, J., Schoemaker, R. C., Chiossi, E., Van Gerven, J., et al. (2010). Orexin receptor antagonism, a new sleep-promoting paradigm: an ascending single-dose study with almorexant. Clin. Pharmacol. Ther. 87, 593-600. doi: 10.1038/clpt.2010.19.
10. Hondo, M., Nagai, K., Ohno, K., Kisanuki, Y., Willie, J. T., Watanabe, T., et al. (2010). Histamine-1 receptor is not required as a downstream effector of orexin-2 receptor in maintenance of basal sleep/wake states. Acta physiol. 198, 287-294. doi: 10.1111/j.1748-1716.2009.02032.x.
11. Hopkins, C. R. (2012). ACS chemical neuroscience molecule spotlight on Suvorexant. ACS Chem. Neurosci. 3, 647-648. doi: 10.1021/cn300086a.
12. Huang, Z. L., Qu, W. M., Li, W. D., Mochizuki, T., Eguchi, N., Watanabe, T., et al. (2001). Arousal effect of orexin A depends on activation of the histaminergic system. Proc. Natl. Acad. Sci. U.S.A. 98, 9965-9970. doi: 10.1073/pnas.181330998.
13. Lee, M. G., Hassani, O. K., and Jones, B. E. (2005). Discharge of identified orexin/hypocretin neurons across the sleep-waking cycle. J. Neurosci. 25, 6716-6720. doi: 10.1523/JNEUROSCI.1887-05.2005.
14. Matsuki, T., Nomiyama, M., Takahira, H., Hirashima, N., Kunita, S., Takahashi, S., et al. (2009). Selective loss of GABA(B) receptors in orexin-producing neurons results in disrupted sleep/wakefulness architecture. Proc. Natl. Acad. Sci. U.S.A. 106, 4459-4464. doi: 10.1073/pnas.0811126106.
15. Mieda, M., Hasegawa, E., Kisanuki, Y. Y., Sinton, C. M., Yanagisawa, M., and Sakurai, T. (2011). Differential roles of orexin receptor-1 and-2 in the regulation of non-REM and REM sleep. J. Neurosci. 31, 6518-6526. doi: 10.1523/JNEUROSCI.6506-10.2011.
16. Mieda, M., and Sakurai, T. (2013). Orexin (hypocretin) receptor agonists and antagonists for treatment of sleep disorders. Rationale for development and current status. CNS Drugs 27, 83-90. doi: 10.1007/s40263-012-0036-8.
17. Mochizuki, T., Arrigoni, E., Marcus, J. N., Clark, E. L., Yamamoto, M., Honer, M., et al. (2011). Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice. Proc. Natl. Acad. Sci. U.S.A. 108, 4471-4476. doi: 10.1073/pnas.1012456108.
18. Morairty, S. R., Revel, F. G., Malherbe, P., Moreau, J. L., Valladao, D., Wettstein, J. G., et al. (2012). Dual hypocretin receptor antagonism is more effective for sleep promotion than antagonism of either receptor alone. PloS ONE 7:e39131. doi: 10.1371/journal.pone.0039131.
19. Neubauer, D. N. (2010). Almorexant, a dual orexin receptor antagonist for the treatment of insomnia. Curr. Opin. Investig. Drugs 11, 101-110.
20. Sakurai, T., and Mieda, M. (2011). Connectomics of orexin-producing neurons: interface of systems of emotion, energy homeostasis and arousal. Trends Pharmacol. Sci. 32, 451-462. doi: 10.1016/j.tips.2011.03.007.
21. Tsujino, N., Tsunematsu, T., Uchigashima, M., Konno, K., Yamanaka, A., Kobayashi, K., et al. (2013). Chronic alterations in monoaminergic cells in the locus coeruleus in orexin neuron-ablated narcoleptic mice. PLoS ONE 8:e70012. doi: 10.1371/journal.pone.0070012.
22. Willie, J. T., Chemelli, R. M., Sinton, C. M., Tokita, S., Williams, S. C., Kisanuki, Y. Y., et al. (2003). Distinct narcolepsy syndromes in Orexin receptor-2 and Orexin null mice: molecular genetic dissection of Non-REM and REM sleep regulatory processes. Neuron 38, 715-730. doi: 10.1016/S0896-6273(03)00330-1.
23. Willie, J. T., Chemelli, R. M., Sinton, C. M., and Yanagisawa, M. (2001). To eat or to sleep? Orexin in the regulation of feeding and wakefulness. Annu. Rev. Neurosci. 24, 429-458. doi: 10.1146/annurev.neuro.24.1.429.
24. Winrow, C. J., Gotter, A. L., Cox, C. D., Tannenbaum, P. L., Garson, S. L., Doran, S. M., et al. (2012). Pharmacological characterization of MK-6096-a dual orexin receptor antagonist for insomnia. Neuropharmacology 62, 978-987. doi: 10.1016/j.neuropharm.2011.10.003.
25. Winrow, C. J., and Renger, J. J. (2013). Discovery and development of orexin receptor antagonists as therapeutics for insomnia. Br. J. Pharmacol. 171, 283-293. doi: 10.1111/bph.12261.
26. Yamanaka, A., Tabuchi, S., Tsunematsu, T., Fukazawa, Y., and Tominaga, M. (2010). Orexin directly excites orexin neurons through orexin 2 receptor. J. Neurosci. 30, 12642-12652. doi: 10.1523/JNEUROSCI.2120-10.2010.
27. Yamanaka, A., Tsujino, N., Funahashi, H., Honda, K., Guan, J. L., Wang, Q. P., et al. (2002). Orexins activate histaminergic neurons via the orexin 2 receptor. Biochem. Biophys. Res. Commun. 290, 1237-1245. doi: 10.1006/bbrc.2001.6318.