ADULT;
ANIMAL EXPERIMENT;
ARTICLE;
CONTROLLED STUDY;
DISSOCIATION CONSTANT;
DRUG DESIGN;
DRUG POTENCY;
DRUG SCREENING;
DRUG SELECTIVITY;
DRUG SYNTHESIS;
HUMAN;
HUMAN CELL;
IN VITRO STUDY;
IN VIVO STUDY;
MALE;
NONHUMAN;
PRIORITY JOURNAL;
RAT;
STRUCTURE ACTIVITY RELATION;
ANIMAL;
CHEMICAL STRUCTURE;
CHEMISTRY;
CHO CELL LINE;
CRICETULUS;
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DRUG EFFECTS;
GENETICS;
LOCOMOTION;
METABOLISM;
PHYSIOLOGY;
SPRAGUE DAWLEY RAT;
SYNTHESIS;
Orexins and orexin receptors: A family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior
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
The hypocretins: Hypothalamus-specific peptides with neuroexcitatory activity
de Lecea, L., Kilduff, T. S., Peyron, C., Gao, X., Foye, P. E., Danielson, P. E., Fukuhara, C., Battenberg, E. L., Gautvik, V. T., Bartlett, F. S., 2nd, Frankel, W. N., van den Pol, A. N., Bloom, F. E., Gautvik, K. M., and Sutcliffe, J. G. (1998) The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity Proc. Natl. Acad. Sci. U. S. A. 95, 322 - 327
Neurons containing hypocretin (orexin) project to multiple neuronal systems
Peyron, C., Tighe, D. K., van den Pol, A. N., de Lecea, L., Heller, H. C., Sutcliffe, J. G., and Kilduff, T. S. (1998) Neurons containing hypocretin (orexin) project to multiple neuronal systems J. Neurosci. 18, 9996 - 10015
Distribution of orexin neurons in the adult rat brain
Nambu, T., Sakurai, T., Mizukami, K., Hosoya, Y., Yanagisawa, M., and Goto, K. (1999) Distribution of orexin neurons in the adult rat brain Brain Res. 827, 243 - 260
Differential expression of orexin receptors 1 and 2 in the rat brain
Marcus, J. N., Aschkenasi, C. J., Lee, C. E., Chemelli, R. M., Saper, C. B., Yanagisawa, M., and Elmquist, J. K. (2001) Differential expression of orexin receptors 1 and 2 in the rat brain J. Comp. Neurol. 435, 6 - 25
Distribution of orexin receptor mRNA in the rat brain
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
Functions of the orexinergic/hypocretinergic system
Kukkonen, J. P., Holmqvist, T., Ammoun, S., and Akerman, K. E. (2002) Functions of the orexinergic/hypocretinergic system Am. J. Physiol.: Cell Physiol. 283, C1567 - 1591
Motivational activation: A unifying hypothesis of orexin/hypocretin function
Mahler, S. V., Moorman, D. E., Smith, R. J., James, M. H., and Aston-Jones, G. (2014) Motivational activation: A unifying hypothesis of orexin/hypocretin function Nat. Neurosci. 17, 1298 - 1303
Orexin/hypocretin: A neuropeptide at the interface of sleep, energy homeostasis, and reward system
Tsujino, N. and Sakurai, T. (2009) Orexin/hypocretin: a neuropeptide at the interface of sleep, energy homeostasis, and reward system Pharmacol. Rev. 61, 162 - 176
Mahler, S. V., Smith, R. J., Moorman, D. E., Sartor, G. C., and Aston-Jones, G. (2012) Multiple roles for orexin/hypocretin in addiction Prog. Brain Res. 198, 79 - 121
Role for hypocretin in mediating stress-induced reinstatement of cocaine-seeking behavior
Boutrel, B., Kenny, P. J., Specio, S. E., Martin-Fardon, R., Markou, A., Koob, G. F., and de Lecea, L. (2005) Role for hypocretin in mediating stress-induced reinstatement of cocaine-seeking behavior Proc. Natl. Acad. Sci. U. S. A. 102, 19168 - 19173
The orexin system regulates alcohol-seeking in rats
Lawrence, A. J., Cowen, M. S., Yang, H. J., Chen, F., and Oldfield, B. (2006) The orexin system regulates alcohol-seeking in rats Br. J. Pharmacol. 148, 752 - 759
Inhibition of orexin-1/hypocretin-1 receptors inhibits yohimbine-induced reinstatement of ethanol and sucrose seeking in Long-Evans rats
Richards, J. K., Simms, J. A., Steensland, P., Taha, S. A., Borgland, S. L., Bonci, A., and Bartlett, S. E. (2008) Inhibition of orexin-1/hypocretin-1 receptors inhibits yohimbine-induced reinstatement of ethanol and sucrose seeking in Long-Evans rats Psychopharmacology 199, 109 - 117
Biomedical application of orexin/hypocretin receptor ligands in neuroscience
Boss, C., Brisbare-Roch, C., and Jenck, F. (2009) Biomedical application of orexin/hypocretin receptor ligands in neuroscience J. Med. Chem. 52, 891 - 903
Orexin receptor antagonists: A new concept in CNS disorders?
Gatfield, J., Brisbare-Roch, C., Jenck, F., and Boss, C. (2010) Orexin receptor antagonists: A new concept in CNS disorders? ChemMedChem 5, 1197 - 1214
Orexin (hypocretin) receptor agonists and antagonists for treatment of sleep disorders. Rationale for development and current status
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
Discovery and development of orexin receptor antagonists as therapeutics for insomnia
Winrow, C. J. and Renger, J. J. (2014) Discovery and development of orexin receptor antagonists as therapeutics for insomnia Br. J. Pharmacol. 171, 283 - 293
SB-334867-A: The first selective orexin-1 receptor antagonist
1179-1182
Smart, D., Sabido-David, C., Brough, S. J., Jewitt, F., Johns, A., Porter, R. A., and Jerman, J. C. (2001) SB-334867-A: The first selective orexin-1 receptor antagonist Br. J. Pharmacol. 132, 1179 - 1182
Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction
WO, Rottapharm S.P.A.
Stasi, P. L. and Rovati, L. (2011) Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction. WO2011006960, Rottapharm S.P.A.
Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists
Gozzi, A., Turrini, G., Piccoli, L., Massagrande, M., Amantini, D., Antolini, M., Martinelli, P., Cesari, N., Montanari, D., Tessari, M., Corsi, M., and Bifone, A. (2011) Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists PloS One 6, e16406
Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist
Steiner, M. A., Gatfield, J., Brisbare-Roch, C., Dietrich, H., Treiber, A., Jenck, F., and Boss, C. (2013) Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist ChemMedChem 8, 898 - 903
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists
Jiang, R., Song, X., Bali, P., Smith, A., Bayona, C. R., Lin, L., Cameron, M. D., McDonald, P. H., Kenny, P. J., and Kamenecka, T. M. (2012) Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists Bioorg. Med. Chem. Lett. 22, 3890 - 3894
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor
Perrey, D. A., German, N. A., Gilmour, B. P., Li, J. X., Harris, D. L., Thomas, B. F., and Zhang, Y. (2013) Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor J. Med. Chem. 56, 6901 - 6916
Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists
Perrey, D. A., Gilmour, B. P., Runyon, S. P., Thomas, B. F., and Zhang, Y. (2011) Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists Bioorg. Med. Chem. Lett. 21, 2980 - 2985
Toward the Development of Bivalent Ligand Probes of Cannabinoid CB1 and Orexin OX1 Receptor Heterodimers
Perrey, D. A., Gilmour, B. P., Thomas, B. F., and Zhang, Y. (2014) Toward the Development of Bivalent Ligand Probes of Cannabinoid CB1 and Orexin OX1 Receptor Heterodimers ACS Med. Chem. Lett. 5, 634 - 638
N -Acyl 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist
Hirose, M., Egashira, S., Goto, Y., Hashihayata, T., Ohtake, N., Iwaasa, H., Hata, M., Fukami, T., Kanatani, A., and 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, 4497 - 4499
Tetrahydroisoquinolines as Orexin Receptor Antagonists: Strategies for Lead Optimization by Solution-Phase Chemistry
Koberstein, R., Aissaoui, H., Bur, D., Clozel, M., Fischli, W., Jenck, F., Mueller, C., Nayler, O., Sifferlen, T., Treiber, A., and Weller, T. (2003) Tetrahydroisoquinolines as Orexin Receptor Antagonists: Strategies for Lead Optimization by Solution-Phase Chemistry Chimia 57, 270 - 275
Orexin A in the VTA is critical for the induction of synaptic plasticity and behavioral sensitization to cocaine
Borgland, S. L., Taha, S. A., Sarti, F., Fields, H. L., and Bonci, A. (2006) Orexin A in the VTA is critical for the induction of synaptic plasticity and behavioral sensitization to cocaine Neuron 49, 589 - 601
The trace amine associated receptor 1 agonist RO5263397 attenuates the induction of cocaine behavioral sensitization in rats
Thorn, D. A., Zhang, C., Zhang, Y., and Li, J. X. (2014) The trace amine associated receptor 1 agonist RO5263397 attenuates the induction of cocaine behavioral sensitization in rats Neurosci. Lett. 566, 67 - 71
Effects of the trace amine-associated receptor 1 agonist RO5263397 on abuse-related effects of cocaine in rats
Thorn, D. A., Jing, L., Qiu, Y., Gancarz-Kausch, A. M., Galuska, C. M., Dietz, D. M., Zhang, Y., and Li, J. X. (2014) Effects of the trace amine-associated receptor 1 agonist RO5263397 on abuse-related effects of cocaine in rats Neuropsychopharmacology 39, 2309 - 2316