1. Akanmu, M. A. and Honda, K. (2005) Selective stimulation of orexin receptor type 2 promotes wakefulness in freely behaving rats.
Brain Res, 1048: 138-145.
[PMID:15919057]
2. Ammoun, S., Holmqvist, T., Shariatmadari, R., Oonk, H. B., Detheux, M., Parmentier, M., Akerman, K. E. and Kukkonen, J. P. (2003) Distinct recognition of OX1 and OX2 receptors by orexin peptides.
J Pharmacol Exp Ther, 305: 507-514.
[PMID:12606634]
3. Asahi, S., Egashira, S., Matsuda, M., Iwaasa, H., Kanatani, A., Ohkubo, M., Ihara, M. and Morishima, H. (2003) Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.
Bioorg Med Chem Lett, 13: 111-113.
[PMID:12467628]
4. Bayer, L., Eggermann, E., Serafin, M., Saint-Mleux, B., Machard, D., Jones, B. and Muhlethaler, M. (2001) Orexins (hypocretins) directly excite tuberomammillary neurons.
Eur J Neurosci, 14: 1571-1575.
[PMID:11722619]
5. Blanco, M., Lopez, M., Garcia-Caballero, T., Gallego, R., Vazquez-Boquete, A., Morel, G., SenarIs, R., Casanueva, F., Dieguez, C. and Beiras, A. (2001) Cellular localization of orexin receptors in human pituitary.
J Clin Endocrinol Metab, 86: 1616-1619.
[PMID:11443222]
6. Brisbare-Roch, C; Dingemanse, J; Koberstein, R; Hoever, P; Aissaoui, H; Flores, S; Mueller, C; Nayler, O; van Gerven, J; de Haas, SL; Hess, P; Qiu, C; Buchmann, S; Scherz, M; Weller, T; Fischli, W; Clozel, M; Jenck, F. (2007) Promotion of sleep by targeting the orexin system in rats, dogs and humans.
Nat. Med., 13 (2): 150-5.
[PMID:17259994]
7. Burdakov, D., Liss, B. and Ashcroft, F. M. (2003) Orexin excites GABAergic neurons of the arcuate nucleus by activating the sodium--calcium exchanger.
J Neurosci, 23: 4951-4957.
[PMID:12832517]
8. Caillol, M., Aioun, J., Baly, C., Persuy, M. A. and Salesse, R. (2003) Localization of orexins and their receptors in the rat olfactory system: possible modulation of olfactory perception by a neuropeptide synthetized centrally or locally.
Brain Res, 960: 48-61.
[PMID:12505657]
9. Chen, J. and Randeva, H. S. (2004) Genomic organization of mouse orexin receptors: characterization of two novel tissue-specific splice variants.
Mol Endocrinol, 18: 2790-2804.
[PMID:15256537]
10. Cluderay, J. E., Harrison, D. C. and Hervieu, G. J. (2002) Protein distribution of the orexin-2 receptor in the rat central nervous system.
Regul Pept, 104: 131-144.
[PMID:11830288]
11. Cox, CD; Breslin, MJ; Whitman, DB; Schreier, JD; McGaughey, GB; Bogusky, MJ; Roecker, AJ; Mercer, SP; Bednar, RA; Lemaire, W; Bruno, JG; Reiss, DR; Harrell, CM; Murphy, KL; Garson, SL; Doran, SM; Prueksaritanont, T; Anderson, WB; Tang, C; Roller, S; Cabalu, TD; Cui, D; Hartman, GD; Young, SD; Koblan, KS; Winrow, CJ; Renger, JJ; Coleman, PJ. (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 (14): 5320-32.
[PMID:20565075]
12. Di Fabio, R; Pellacani, A; Faedo, S; Roth, A; Piccoli, L; Gerrard, P; Porter, RA; Johnson, CN; Thewlis, K; Donati, D; et al.. (2011) Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Bioorg. Med. Chem. Lett., 21 (18): 5562-7.
[PMID:21831639]
13. Eggermann, E., Serafin, M., Bayer, L., Machard, D., Saint-Mleux, B., Jones, B. E. and Muhlethaler, M. (2001) Orexins/hypocretins excite basal forebrain cholinergic neurones.
Neuroscience, 108: 177-181.
[PMID:11734353]
14. Eriksson, K. S., Sergeeva, O., Brown, R. E. and Haas, H. L. (2001) Orexin/hypocretin excites the histaminergic neurons of the tuberomammillary nucleus.
J Neurosci, 21: 9273-9279.
[PMID:11717361]
15. Hirose, M; Egashira, S; Goto, Y; Hashihayata, T; Ohtake, N; Iwaasa, H; Hata, M; Fukami, T; Kanatani, A; Yamada, K. (2003) N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.
Bioorg. Med. Chem. Lett., 13 (24): 4497-9.
[PMID:14643355]
16. Hirota, K., Kushikata, T., Kudo, M., Kudo, T., Lambert, D. G. and Matsuki, A. (2001) Orexin A and B evoke noradrenaline release from rat cerebrocortical slices.
Br J Pharmacol, 134: 1461-1466.
[PMID:11724752]
17. Hoang, Q. V., Bajic, D., Yanagisawa, M., Nakajima, S. and Nakajima, Y. (2003) Effects of orexin (hypocretin) on GIRK channels.
J Neurophysiol, 90: 693-702.
[PMID:12702704]
18. Holmqvist, T., Akerman, K. E. and Kukkonen, J. P. (2001) High specificity of human orexin receptors for orexins over neuropeptide Y and other neuropeptides.
Neurosci Lett, 305: 177-180.
[PMID:11403934]
19. Holmqvist, T., Johansson, L., Ostman, M., Ammoun, S., Akerman, K. E. and Kukkonen, J. P. (2005) OX1 orexin receptors couple to adenylyl cyclase regulation via multiple mechanisms.
J Biol Chem, 280: 6570-6579.
[PMID:15611118]
20. Holmqvist, T; Akerman, KE; Kukkonen, JP. (2002) Orexin signaling in recombinant neuron-like cells.
FEBS Lett., 526 (1-3): 11-4.
[PMID:12208495]
21. Ishibashi, M., Takano, S., Yanagida, H., Takatsuna, M., Nakajima, K., Oomura, Y., Wayner, M. J. and Sasaki, K. (2005) Effects of orexins/hypocretins on neuronal activity in the paraventricular nucleus of the thalamus in rats in vitro.
Peptides, 26: 471-481.
[PMID:15652654]
22. Langmead, C. J., Jerman, J. C., Brough, S. J., Scott, C., Porter, R. A. and Herdon, H. J. (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Br J Pharmacol, 141: 340-346.
[PMID:14691055]
23. Lopez, M., SenarIs, R., Gallego, R., Garcia-Caballero, T., Lago, F., Seoane, L., Casanueva, F. and Dieguez, C. (1999) Orexin receptors are expressed in the adrenal medulla of the rat.
Endocrinology, 140: 5991-5994.
[PMID:10579367]
24. Malherbe, P; Borroni, E; Gobbi, L; Knust, H; Nettekoven, M; Pinard, E; Roche, O; Rogers-Evans, M; Wettstein, JG; Moreau, JL. (2009) Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.
Br. J. Pharmacol., 156 (8): 1326-41.
[PMID:19751316]
25. Malherbe, P; Borroni, E; Pinard, E; Wettstein, JG; Knoflach, F. (2009) Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.
Mol. Pharmacol., 76 (3): 618-31.
[PMID:19542319]
26. McAtee, L. C., Sutton, S. W., Rudolph, D. A., Li, X., Aluisio, L. E., Phuong, V. K., Dvorak, C. A., Lovenberg, T. W., Carruthers, N. I. and Jones, T. K. (2004) Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.
Bioorg Med Chem Lett, 14: 4225-4229.
[PMID:15261275]
27. Mikkelsen, J. D., Hauser, F., deLecea, L., Sutcliffe, J. G., Kilduff, T. S., Calgari, C., Pevet, P. and Simonneaux, V. (2001) Hypocretin (orexin) in the rat pineal gland: a central transmitter with effects on noradrenaline-induced release of melatonin.
Eur J Neurosci, 14: 419-425.
[PMID:11553292]
28. Nowak, K. W., Strowski, M. Z., Switonska, M. M., Kaczmarek, P., Singh, V., Fabis, M., Mackowiak, P., Nowak, M. and Malendowicz, L. K. (2005) Evidence that orexins A and B stimulate insulin secretion from rat pancreatic islets via both receptor subtypes.
Int J Mol Med, 15: 969-972.
[PMID:15870901]
29. Okumura, T; Takeuchi, S; Motomura, W; Yamada, H; Egashira Si, S; Asahi, S; Kanatani, A; Ihara, M; Kohgo, Y. (2001) Requirement of intact disulfide bonds in orexin-A-induced stimulation of gastric acid secretion that is mediated by OX1 receptor activation.
Biochem. Biophys. Res. Commun., 280 (4): 976-81.
[PMID:11162621]
30. Porter, R. A., Chan, W. N., Coulton, S., Johns, A., Hadley, M. S., Widdowson, K., Jerman, J. C., Brough, S. J., Coldwell, M., Smart, D., Jewitt, F., Jeffrey, P. and Austin, N. (2001) 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Bioorg Med Chem Lett, 11: 1907-1910.
[PMID:11459658]
31. Putula, J; Turunen, PM; Jäntti, MH; Ekholm, ME; Kukkonen, JP. (2011) Agonist ligand discrimination by the two orexin receptors depends on the expression system.
Neurosci. Lett., 494 (1): 57-60.
[PMID:21362456]
32. Rainero, I., Gallone, S., Valfre, W., Ferrero, M., Angilella, G., Rivoiro, C., Rubino, E., De Martino, P., Savi, L., Ferrone, M. and Pinessi, L. (2004) A polymorphism of the hypocretin receptor 2 gene is associated with cluster headache.
Neurology, 63: 1286-1288.
[PMID:15477554]
33. Sakurai, T., Amemiya, A., Ishii, M., Matsuzaki, I., Chemelli, R. M., Tanaka, H., Williams, S. C., Richardson, J. A., Kozlowski, G. P., Wilson, S., Arch, J. R., Buckingham, R. E., Haynes, A. C., Carr, S. A., Annan, R. S., McNulty, D. E., Liu, W. S., Terrett, J. A., Elshourbagy, N. A., Bergsma, D. J. and Yanagisawa, M. (1998) Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.
Cell, 92: 573-585.
[PMID:9491897]
34. Seoane, L. M., Tovar, S. A., Perez, D., Mallo, F., Lopez, M., SenarIs, R., Casanueva, F. F. and Dieguez, C. (2004) Orexin A suppresses in vivo GH secretion.
Eur J Endocrinol, 150: 731-736.
[PMID:15132732]
35. Shoblock, JR; Welty, N; Aluisio, L; Fraser, I; Motley, ST; Morton, K; Palmer, J; Bonaventure, P; Carruthers, NI; Lovenberg, TW; et al.. (2011) Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement.
Psychopharmacology (Berl.), 215 (1): 191-203.
[PMID:21181123]
36. Smart, D., Jerman, J. C., Brough, S. J., Rushton, S. L., Murdock, P. R., Jewitt, F., Elshourbagy, N. A., Ellis, C. E., Middlemiss, D. N. and Brown, F. (1999) Characterization of recombinant human orexin receptor pharmacology in a Chinese hamster ovary cell-line using FLIPR.
Br J Pharmacol, 128: 1-3.
[PMID:10498827]
37. Sunter, D., Morgan, I., Edwards, C. M., Dakin, C. L., Murphy, K. G., Gardiner, J., Taheri, S., Rayes, E. and Bloom, S. R. (2001) Orexins: effects on behavior and localisation of orexin receptor 2 messenger ribonucleic acid in the rat brainstem.
Brain Res, 907: 27-34.
[PMID:11430882]
38. Tang, J; Chen, J; Ramanjaneya, M; Punn, A; Conner, AC; Randeva, HS. (2008) The signalling profile of recombinant human orexin-2 receptor.
Cell. Signal., 20 (9): 1651-61.
[PMID:18599270]
39. Trivedi, P., Yu, H., MacNeil, D. J., Van der Ploeg, L. H. and Guan, X. M. (1998) Distribution of orexin receptor mRNA in the rat brain.
FEBS Lett, 438: 71-75.
[PMID:9821961]
40. Voisin, T; Firar, AE; Avondo, V; Laburthe, M. (2006) Orexin-induced apoptosis: the key role of the seven-transmembrane domain orexin type 2 receptor.
Endocrinology, 147 (10): 4977-84.
[PMID:16857748]
41. Willie, J. T., Chemelli, R. M., Sinton, C. M., Tokita, S., Williams, S. C., Kisanuki, Y. Y., Marcus, J. N., Lee, C., Elmquist, J. K., Kohlmeier, K. A., Leonard, C. S., Richardson, J. A., Hammer, R. E. and Yanagisawa, M. (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.
[PMID:12797957]
42. Winrow, CJ; Gotter, AL; Cox, CD; Tannenbaum, PL; Garson, SL; Doran, SM; Breslin, MJ; Schreier, JD; Fox, SV; Harrell, CM; et al.. (2012) Pharmacological characterization of MK-6096 - A dual orexin receptor antagonist for insomnia.
Neuropharmacology, 62 (2): 978-87.
[PMID:22019562]
43. Wu, M., Zhang, Z., Leranth, C., Xu, C., Van den Pol, A. N. and Alreja, M. (2002) Hypocretin increases impulse flow in the septohippocampal GABAergic pathway: implications for arousal via a mechanism of hippocampal disinhibition.
J Neurosci, 22: 7754-7765.
[PMID:12196599]
44. Zhu, Y., Miwa, Y., Yamanaka, A., Yada, T., Shibahara, M., Abe, Y., Sakurai, T. and Goto, K. (2003) Orexin receptor type-1 couples exclusively to pertussis toxin-insensitive G-proteins, while orexin receptor type-2 couples to both pertussis toxin-sensitive and -insensitive G-proteins.
J Pharmacol Sci, 92: 259-266.
[PMID:12890892]