메뉴 건너뛰기




Volumn 11, Issue 6, 2011, Pages 696-725

Discovery of Dual Orexin Receptor Antagonists (DORAs) for the Treatment of Insomnia

Author keywords

Brain penetration; Diazepane; G protein coupled receptor; Insomnia; Neuropeptide; Orexin; Sleep

Indexed keywords

ALMOREXANT; JNJ 1037049; OREXIN; OREXIN 1 RECEPTOR; OREXIN 2 RECEPTOR; OREXIN RECEPTOR BLOCKING AGENT; RECEPTOR BLOCKING AGENT; SB 649868; UNCLASSIFIED DRUG;

EID: 79952946685     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/1568026611109060696     Document Type: Review
Times cited : (40)

References (59)
  • 4
    • 65949100369 scopus 로고    scopus 로고
    • Hypocretin/orexin neuropeptides: Participation in the control of sleep-wakefulness cycle and energy homeostasis
    • Nunez, A.; Rodrigo-Angulo, M. L.; de Andres, I.; Garzon, M. Hypocretin/orexin neuropeptides: participation in the control of sleep-wakefulness cycle and energy homeostasis. Curr. Neuropharmacol., 2009, 7(1), 50-59.
    • (2009) Curr. Neuropharmacol , vol.7 , Issue.1 , pp. 50-59
    • Nunez, A.1    Rodrigo-Angulo, M.L.2    de Andres, I.3    Garzon, M.4
  • 5
    • 34248149838 scopus 로고    scopus 로고
    • Clinical and neurobiological aspects of narcolepsy
    • Nishino, S. Clinical and neurobiological aspects of narcolepsy. Sleep Med., 2007, 8 (4), 373-399.
    • (2007) Sleep Med , vol.8 , Issue.4 , pp. 373-399
    • Nishino, S.1
  • 9
    • 0032142849 scopus 로고    scopus 로고
    • Development of cataplexy in genetically narcoleptic dobermans
    • Riehl, J.; Nishino, S.; Cederberg, R.; Dement, W. C.; Mignot, E. Development of cataplexy in genetically narcoleptic dobermans. Exp. Neurol., 1998, 152(2), 292-302.
    • (1998) Exp. Neurol , vol.152 , Issue.2 , pp. 292-302
    • Riehl, J.1    Nishino, S.2    Cederberg, R.3    Dement, W.C.4    Mignot, E.5
  • 13
    • 48249109864 scopus 로고    scopus 로고
    • Orexin receptor antagonists: Medici-nal chemistry and therapeutic potential
    • Roecker, A. J.; Coleman, P. J. Orexin receptor antagonists: medici-nal chemistry and therapeutic potential. Curr. Top. Med. Chem., 2008,8(11), 977-987.
    • (2008) Curr. Top. Med. Chem , vol.8 , Issue.11 , pp. 977-987
    • Roecker, A.J.1    Coleman, P.J.2
  • 15
    • 0042565939 scopus 로고    scopus 로고
    • Orexin receptor type-1 couples exclu-sively to pertussis toxin-insensitive G-proteins, while orexin recep-tor type-2 couples to both pertussis toxin-sensitive and -insensitive G-proteins
    • Zhu, Y.; Miwa, Y.; Yamanaka, A.; Yada, T.; Shibahara, M.; Abe, Y.; Sakurai, T.; Goto, K. Orexin receptor type-1 couples exclu-sively to pertussis toxin-insensitive G-proteins, while orexin recep-tor type-2 couples to both pertussis toxin-sensitive and -insensitive G-proteins. J. Pharmacol. Sci., 2003, 92(3), 259-266.
    • (2003) J. Pharmacol. Sci , vol.92 , Issue.3 , pp. 259-266
    • Zhu, Y.1    Miwa, Y.2    Yamanaka, A.3    Yada, T.4    Shibahara, M.5    Abe, Y.6    Sakurai, T.7    Goto, K.8
  • 17
    • 30944459667 scopus 로고    scopus 로고
    • Hypocretin/orexin selectively in-creases dopamine efflux within the prefrontal cortex: Involvement of the ventral tegmental area
    • Vittoz, N. M.; Berridge, C.W. Hypocretin/orexin selectively in-creases dopamine efflux within the prefrontal cortex: Involvement of the ventral tegmental area. Neuropsychopharmacology, 2006, 31(2), 384-395.
    • (2006) Neuropsychopharmacology , vol.31 , Issue.2 , pp. 384-395
    • Vittoz, N.M.1    Berridge, C.W.2
  • 18
    • 0242456105 scopus 로고    scopus 로고
    • Hypocretin-1 causes G protein activation and increases ACh release in rat pons
    • Bernard, R.; Lydic, R.; Baghdoyan, H. A. Hypocretin-1 causes G protein activation and increases ACh release in rat pons. Eur. J. Neurosci., 2003, 18 (7), 1775-1785.
    • (2003) Eur. J. Neurosci , vol.18 , Issue.7 , pp. 1775-1785
    • Bernard, R.1    Lydic, R.2    Baghdoyan, H.A.3
  • 19
    • 68049135722 scopus 로고    scopus 로고
    • Nutritional status modulates be-havioral and olfactory bulb Fos responses to isoamyl acetate or food odour in rats: Roles of orexins and leptin
    • Prud'homme, M. J.; Lacroix, M. C.; Badonnel, K.; Gougis, S.; Baly, C.; Salesse, R.; Caillol, M. Nutritional status modulates be-havioral and olfactory bulb Fos responses to isoamyl acetate or food odour in rats: roles of orexins and leptin. Neuroscience, 2009, 162(4), 1287-1298.
    • (2009) Neuroscience , vol.162 , Issue.4 , pp. 1287-1298
    • Prud'homme, M.J.1    Lacroix, M.C.2    Badonnel, K.3    Gougis, S.4    Baly, C.5    Salesse, R.6    Caillol, M.7
  • 20
    • 67349114404 scopus 로고    scopus 로고
    • Orexin-A and ghrelin depolarize the same pedunculopontine teg-mental neurons in rats: An in vitro study
    • Kim, J.; Nakajima, K.; Oomura, Y.; Wayner, M. J.; Sasaki, K. Orexin-A and ghrelin depolarize the same pedunculopontine teg-mental neurons in rats: An in vitro study. Peptides, 2009, 30(7), 1328-1335.
    • (2009) Peptides , vol.30 , Issue.7 , pp. 1328-1335
    • Kim, J.1    Nakajima, K.2    Oomura, Y.3    Wayner, M.J.4    Sasaki, K.5
  • 22
    • 77649157819 scopus 로고    scopus 로고
    • Orexin Receptor Antagonists: A re-view of promising compounds patented since 2006
    • Coleman, P. J.; Renger, J. J.; Orexin Receptor Antagonists: A re-view of promising compounds patented since 2006. Expert Opin. Ther. Pat., 2010, 20(3),307-324
    • (2010) Expert Opin. Ther. Pat , vol.20 , Issue.3 , pp. 307-324
    • Coleman, P.J.1    Renger, J.J.2
  • 27
    • 18144389456 scopus 로고    scopus 로고
    • Orexin-A (hypocretin-1) is possibly involved in generation of anxi-ety-like behavior
    • Suzuki, M.; Beuckmann, C. T.; Shikata, K.; Ogura, H.; Sawai, T. Orexin-A (hypocretin-1) is possibly involved in generation of anxi-ety-like behavior. Brain Res., 2005, 1044(1), 116-121.
    • (2005) Brain Res , vol.1044 , Issue.1 , pp. 116-121
    • Suzuki, M.1    Beuckmann, C.T.2    Shikata, K.3    Ogura, H.4    Sawai, T.5
  • 28
    • 50249149817 scopus 로고    scopus 로고
    • Changes in brain orexin levels in a rat model of depression induced by neonatal ad-ministration of clomipramine
    • Feng, P.; Vurbic, D.; Wu, Z.; Hu, Y.; Strohl, K. P. Changes in brain orexin levels in a rat model of depression induced by neonatal ad-ministration of clomipramine. J. Psychopharmacol., 2008, 22(7), 784-791.
    • (2008) J. Psychopharmacol , vol.22 , Issue.7 , pp. 784-791
    • Feng, P.1    Vurbic, D.2    Wu, Z.3    Hu, Y.4    Strohl, K.P.5
  • 29
    • 25644432796 scopus 로고    scopus 로고
    • A role for lateral hypothalamic orexin neurons in reward seeking
    • Harris, G. C.; Wimmer, M.; Aston-Jones, G. A role for lateral hypothalamic orexin neurons in reward seeking. Nature, 2005, 437, 556-559.
    • (2005) Nature , vol.437 , pp. 556-559
    • Harris, G.C.1    Wimmer, M.2    Aston-Jones, G.3
  • 34
    • 79952939664 scopus 로고    scopus 로고
    • Diazaspi-rodecane orexin receptor antagonists
    • WO 2007025069
    • Breslin, M. J.; Cox, Christopher D.; Whitman, David B. Diazaspi-rodecane orexin receptor antagonists. PCT Int. Appl., WO 2007025069, 2007.
    • (2007) PCT Int. Appl
    • Breslin, M.J.1    Cox, C.D.2    Whitman, D.B.3
  • 35
    • 79952962491 scopus 로고    scopus 로고
    • Preparation of indole compounds containing an oxazole moiety as orexin receptor an-tagonists
    • WO 2007061763A1
    • Bergman, J.M.; Coleman, P.J.; Roecker, A.J. Preparation of indole compounds containing an oxazole moiety as orexin receptor an-tagonists. PCT Int. Appl., WO 2007061763A1. 2007.
    • (2007) PCT Int. Appl
    • Bergman, J.M.1    Coleman, P.J.2    Roecker, A.J.3
  • 36
    • 33845432139 scopus 로고    scopus 로고
    • Electrophilic intermediates produced by bioacti-vation of furan
    • Peterson, L.A. Electrophilic intermediates produced by bioacti-vation of furan. Drug Met. Rev., 2006, 38, 615-626.
    • (2006) Drug Met. Rev , vol.38 , pp. 615-626
    • Peterson, L.A.1
  • 37
    • 0029882427 scopus 로고    scopus 로고
    • Microsomal metabolism of the 5-lipoxygenase inhibitor L-739,010: Evidence for furan bioac-tivation
    • Zhang, K. E.; Naue, J. A.; Arison, B.; Vyas, K. P. Microsomal metabolism of the 5-lipoxygenase inhibitor L-739,010: Evidence for furan bioac-tivation. Chem. Res. Toxicol., 1996, 9, 547-554.
    • (1996) Chem. Res. Toxicol , vol.9 , pp. 547-554
    • Zhang, K.E.1    Naue, J.A.2    Arison, B.3    Vyas, K.P.4
  • 40
    • 0026976875 scopus 로고
    • Subacute toxic-ity of a halogenated pyrrole hydroxymethylglutaryl-coenzyme A reductase inhibitor in Wistar rats
    • Sigler, R. E.; Dominick, M. A.; McGuire, E. J. Subacute toxic-ity of a halogenated pyrrole hydroxymethylglutaryl-coenzyme A reductase inhibitor in Wistar rats. Toxicol. Pathol., 1992, 20, 595-602.
    • (1992) Toxicol. Pathol , vol.20 , pp. 595-602
    • Sigler, R.E.1    Dominick, M.A.2    McGuire, E.J.3
  • 41
    • 0024078378 scopus 로고
    • Toxicity and metabolism of pyrrolizidine al-kaloids
    • Cheeke, P. R. Toxicity and metabolism of pyrrolizidine al-kaloids. J. Amin. Sci., 1988, 66, 2343-2350.
    • (1988) J. Amin. Sci , vol.66 , pp. 2343-2350
    • Cheeke, P.R.1
  • 42
    • 85088738372 scopus 로고    scopus 로고
    • These CYP-related issue were representative of the proline bis-amide series of orexin an-tagonists
    • Compound 5-14 demonstrated an IC50 = 2.5 M against CYP 3A4 and an EC50 = 1.9 M inducing hPXR. These CYP-related issue were representative of the proline bis-amide series of orexin an-tagonists.
    • 50 = 2.5 M Against CYP 3A4 and An EC50 = 1.9 M Inducing HPXR
  • 43
    • 79952905926 scopus 로고    scopus 로고
    • Preparation of N-aroyl cyclic amines as orexin receptor antago-nists
    • WO 2002089800 A2
    • Gaillard, Pascale; Johnson, Christopher Norbert; Novelli, Riccardo; Porter, Roderick Alan; Stemp, Geoffrey; Thewlis, Kevin Michael. Preparation of N-aroyl cyclic amines as orexin receptor antago-nists. PCT Int. Appl., WO 2002089800 A2. 2002.
    • (2002) PCT Int. Appl
    • Gaillard, P.1    Johnson, C.N.2    Novelli, R.3    Alan, P.R.4    Stemp, G.5    Michael, T.K.6
  • 44
    • 79952933757 scopus 로고    scopus 로고
    • Preparation of amidopropoxyphenyl compounds as orexin receptor antagonists for treating neurological and psychiatric disorders
    • WO 2006110626
    • Coleman, P. J.; Schreier, J. Preparation of amidopropoxyphenyl compounds as orexin receptor antagonists for treating neurological and psychiatric disorders. PCT Int. Appl., WO 2006110626. 2006, A1.
    • (2006) PCT Int. Appl
    • Coleman, P.J.1    Schreier, J.2
  • 45
    • 70350516326 scopus 로고    scopus 로고
    • Utility of unbound plasma drug levels and P-glycoprotein transport data in prediction of central nervous system exposure
    • He, H.; Lyons, K. A.; Shen, X.; Yao, Z.; Bleasby, K.; Chan, G.; Hafey, M.; Li, X.; Xu, S.; Salituro, G. M.; Cohen, L. H.; Tang, W. Utility of unbound plasma drug levels and P-glycoprotein transport data in prediction of central nervous system exposure. Xenobiotica, 2009,39(9), 687-693.
    • (2009) Xenobiotica , vol.39 , Issue.9 , pp. 687-693
    • He, H.1    Lyons, K.A.2    Shen, X.3    Yao, Z.4    Bleasby, K.5    Chan, G.6    Hafey, M.7    Li, X.8    Xu, S.9    Salituro, G.M.10    Cohen, L.H.11    Tang, W.12
  • 46
    • 38849136513 scopus 로고    scopus 로고
    • CSF as a surrogate for assessing CNS exposure: An in-dustrial perspective
    • Lin, J. H. CSF as a surrogate for assessing CNS exposure: an in-dustrial perspective. Curr. Drug Metabol., 2008, 9(1), 46-59.
    • (2008) Curr. Drug Metabol , vol.9 , Issue.1 , pp. 46-59
    • Lin, J.H.1
  • 47
    • 79952912114 scopus 로고    scopus 로고
    • Amidoethyl alkylamino orexin recep-tor antagonists
    • WO 2009011775A1
    • Coleman, P. J.; Schreier, J.D. Amidoethyl alkylamino orexin recep-tor antagonists. PCT Int. Appl., WO 2009011775A1. 2009.
    • (2009) PCT Int. Appl
    • Coleman, P.J.1    Schreier, J.D.2
  • 48
    • 0037030653 scopus 로고    scopus 로고
    • Molecular properties that influence the oral bioavailability of drug candidates
    • Veber, D. F.; Johnson, S. R.; Cheng, H.-Y.; Smith, B. R.; Ward, K. W.; Kopple, K. D. Molecular properties that influence the oral bioavailability of drug candidates. J. Med. Chem., 2002, 45(12), 2615-2623.
    • (2002) J. Med. Chem , vol.45 , Issue.12 , pp. 2615-2623
    • Veber, D.F.1    Johnson, S.R.2    Cheng, H.-Y.3    Smith, B.R.4    Ward, K.W.5    Kopple, K.D.6
  • 50
    • 79952931673 scopus 로고    scopus 로고
    • Substituted diazepane orexin receptor antagonists
    • WO 2008008518
    • Cox, C. D.; Breslin, M. J.; Coleman, P. J. Substituted diazepane orexin receptor antagonists. PCT Int. Appl., WO 2008008518. 2008.
    • (2008) PCT Int. Appl
    • Cox, C.D.1    Breslin, M.J.2    Coleman, P.J.3
  • 55
    • 79952959503 scopus 로고    scopus 로고
    • Preparation of bridged diazepane com-pounds as orexin receptor antagonists
    • WO 2008008517
    • Coleman, P. J.; Cox, Christopher D.; McGaughey, G. B.; Ro-ecker, A. J.; Schreier, J. D. Preparation of bridged diazepane com-pounds as orexin receptor antagonists. PCT Int. Appl., WO 2008008517. 2008.
    • (2008) PCT Int. Appl
    • Coleman, P.J.1    Cox, C.D.2    McGaughey, G.B.3    Ro-ecker, A.J.4    Schreier, J.D.5
  • 57
    • 79952917752 scopus 로고    scopus 로고
    • Three atom bridges containing an oxygen atom were also made and found to be potent DORAs; see: Cox, Christopher D.; Whitman, David B. Oxo bridged diazepane orexin receptor antagonists
    • WO 2008143856
    • Three atom bridges containing an oxygen atom were also made and found to be potent DORAs; see: Cox, Christopher D.; Whitman, David B. Oxo bridged diazepane orexin receptor antagonists. PCT Int. Appl., 2008 WO 2008143856.
    • (2008) PCT Int. Appl


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.