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Items: 1 to 50 of 96

1.

Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure-Activity Relationships, and Sleep-Promoting Properties in Rats.

Brotschi C, Roch C, Gatfield J, Treiber A, Williams JT, Sifferlen T, Heidmann B, Jenck F, Bolli MH, Boss C.

ChemMedChem. 2019 Jul 3;14(13):1257-1270. doi: 10.1002/cmdc.201900242. Epub 2019 Jun 5.

PMID:
31066976
2.

The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468.

Treiber A, de Kanter R, Roch C, Gatfield J, Boss C, von Raumer M, Schindelholz B, Muehlan C, van Gerven J, Jenck F.

J Pharmacol Exp Ther. 2017 Sep;362(3):489-503. doi: 10.1124/jpet.117.241596. Epub 2017 Jun 29.

PMID:
28663311
3.

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach.

Heidmann B, Gatfield J, Roch C, Treiber A, Tortoioli S, Brotschi C, Williams JT, Bolli MH, Abele S, Sifferlen T, Jenck F, Boss C.

ChemMedChem. 2016 Oct 6;11(19):2132-2146. doi: 10.1002/cmdc.201600175. Epub 2016 Jul 8.

PMID:
27390287
4.

Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.

Sifferlen T, Boller A, Chardonneau A, Cottreel E, Gatfield J, Treiber A, Roch C, Jenck F, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Boss C.

Bioorg Med Chem Lett. 2015 May 1;25(9):1884-91. doi: 10.1016/j.bmcl.2015.03.035. Epub 2015 Mar 21.

PMID:
25838147
5.

Orexin neuropeptides contribute to the development and persistence of generalized avoidance behavior in the rat.

Viviani D, Haegler P, Jenck F, Steiner MA.

Psychopharmacology (Berl). 2015 Apr;232(8):1383-93. doi: 10.1007/s00213-014-3769-x. Epub 2014 Oct 16.

PMID:
25319964
6.

Structure-activity relationship, biological, and pharmacological characterization of the proline sulfonamide ACT-462206: a potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.

Boss C, Roch-Brisbare C, Steiner MA, Treiber A, Dietrich H, Jenck F, von Raumer M, Sifferlen T, Brotschi C, Heidmann B, Williams JT, Aissaoui H, Siegrist R, Gatfield J.

ChemMedChem. 2014 Nov;9(11):2486-96. doi: 10.1002/cmdc.201402258. Epub 2014 Aug 21.

PMID:
25147058
7.

Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1.

Sifferlen T, Boller A, Chardonneau A, Cottreel E, Hoecker J, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Gatfield J, Treiber A, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1201-8. doi: 10.1016/j.bmcl.2013.12.092. Epub 2013 Dec 30.

PMID:
24447850
8.

The selective orexin receptor 1 antagonist ACT-335827 in a rat model of diet-induced obesity associated with metabolic syndrome.

Steiner MA, Sciarretta C, Pasquali A, Jenck F.

Front Pharmacol. 2013 Dec 30;4:165. doi: 10.3389/fphar.2013.00165. eCollection 2013.

9.

Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.

Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3857-63. doi: 10.1016/j.bmcl.2013.04.071. Epub 2013 May 8.

PMID:
23719231
10.

Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist.

Steiner MA, Gatfield J, Brisbare-Roch C, Dietrich H, Treiber A, Jenck F, Boss C.

ChemMedChem. 2013 Jun;8(6):898-903. doi: 10.1002/cmdc.201300003. Epub 2013 Apr 15.

PMID:
23589487
11.

Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1.

Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2212-6. doi: 10.1016/j.bmcl.2013.01.088. Epub 2013 Jan 29.

PMID:
23434414
12.

Examining the role of endogenous orexins in hypothalamus-pituitary-adrenal axis endocrine function using transient dual orexin receptor antagonism in the rat.

Steiner MA, Sciarretta C, Brisbare-Roch C, Strasser DS, Studer R, Jenck F.

Psychoneuroendocrinology. 2013 Apr;38(4):560-71. doi: 10.1016/j.psyneuen.2012.07.016. Epub 2012 Aug 20.

PMID:
22917622
13.

The brain orexin system and almorexant in fear-conditioned startle reactions in the rat.

Steiner MA, Lecourt H, Jenck F.

Psychopharmacology (Berl). 2012 Oct;223(4):465-75. Epub 2012 May 17.

PMID:
22592903
14.

The dual orexin receptor antagonist almorexant, alone and in combination with morphine, cocaine and amphetamine, on conditioned place preference and locomotor sensitization in the rat.

Steiner MA, Lecourt H, Jenck F.

Int J Neuropsychopharmacol. 2013 Mar;16(2):417-32. doi: 10.1017/S1461145712000193. Epub 2012 Mar 21.

PMID:
22436395
15.

Favoured genetic background for testing anxiolytics in the fear-potentiated and light-enhanced startle paradigms in the rat.

Steiner MA, Lecourt H, Rakotoariniaina A, Jenck F.

Behav Brain Res. 2011 Aug 1;221(1):34-42. doi: 10.1016/j.bbr.2011.02.021. Epub 2011 Feb 24.

PMID:
21354212
16.

Differential effects of the dual orexin receptor antagonist almorexant and the GABA(A)-α1 receptor modulator zolpidem, alone or combined with ethanol, on motor performance in the rat.

Steiner MA, Lecourt H, Strasser DS, Brisbare-Roch C, Jenck F.

Neuropsychopharmacology. 2011 Mar;36(4):848-56. doi: 10.1038/npp.2010.224. Epub 2010 Dec 8.

17.

Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant.

Dietrich H, Jenck F.

Psychopharmacology (Berl). 2010 Oct;212(2):145-54. doi: 10.1007/s00213-010-1933-5. Epub 2010 Jul 15.

18.

Orexin receptor antagonists: a new concept in CNS disorders?

Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

ChemMedChem. 2010 Aug 2;5(8):1197-214. doi: 10.1002/cmdc.201000132. Review. No abstract available.

PMID:
20544785
19.

Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.

Sifferlen T, Boss C, Cottreel E, Koberstein R, Gude M, Aissaoui H, Weller T, Gatfield J, Brisbare-Roch C, Jenck F.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1539-42. doi: 10.1016/j.bmcl.2010.01.070. Epub 2010 Jan 22.

PMID:
20144866
20.

Biomedical application of orexin/hypocretin receptor ligands in neuroscience.

Boss C, Brisbare-Roch C, Jenck F.

J Med Chem. 2009 Feb 26;52(4):891-903. doi: 10.1021/jm801296d. Review. No abstract available.

PMID:
19199652
21.

N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.

Aissaoui H, Koberstein R, Zumbrunn C, Gatfield J, Brisbare-Roch C, Jenck F, Treiber A, Boss C.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5729-33. doi: 10.1016/j.bmcl.2008.09.079. Epub 2008 Sep 26.

PMID:
18845436
22.

Promotion of sleep by targeting the orexin system in rats, dogs and humans.

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.

Nat Med. 2007 Feb;13(2):150-5. Epub 2007 Jan 28.

PMID:
17259994
23.

The role of 5-HT2C receptors in affective disorders.

Jenck F, Bös M, Wichmann J, Stadler H, Martin JR, Moreau JL.

Expert Opin Investig Drugs. 1998 Oct;7(10):1587-99.

PMID:
15991903
24.

Impact of environmental housing conditions on the emotional responses of mice deficient for nociceptin/orphanin FQ peptide precursor gene.

Ouagazzal AM, Moreau JL, Pauly-Evers M, Jenck F.

Behav Brain Res. 2003 Sep 15;144(1-2):111-7.

PMID:
12946601
25.

Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.

Kolczewski S, Adam G, Cesura AM, Jenck F, Hennig M, Oberhauser T, Poli SM, Rössler F, Röver S, Wichmann J, Dautzenberg FM.

J Med Chem. 2003 Jan 16;46(2):255-64.

PMID:
12519064
26.
27.

Reversal of stress- and CRF-induced anorexia in rats by the synthetic nociceptin/orphanin FQ receptor agonist, Ro 64-6198.

Ciccocioppo R, Biondini M, Antonelli L, Wichmann J, Jenck F, Massi M.

Psychopharmacology (Berl). 2002 May;161(2):113-9. Epub 2002 Mar 22.

PMID:
11981590
28.

The orphanin receptor agonist RO 64-6198 does not induce place conditioning in rats.

Le Pen G, Wichmann J, Moreau JL, Jenck F.

Neuroreport. 2002 Mar 25;13(4):451-4.

PMID:
11930159
29.

A combined pharmacological and genetic approach to investigate the role of orphanin FQ in learning and memory.

Higgins GA, Kew JN, Richards JG, Takeshima H, Jenck F, Adam G, Wichmann J, Kemp JA, Grottick AJ.

Eur J Neurosci. 2002 Mar;15(5):911-22.

PMID:
11906533
30.

Improved Semliki Forest virus vectors for receptor research and gene therapy.

Lundstrom K, Ziltener P, Hermann D, Schweitzer C, Richards JG, Jenck F.

J Recept Signal Transduct Res. 2001 Feb;21(1):55-70.

PMID:
11693173
31.

Drug-induced potentiation of prepulse inhibition of acoustic startle reflex in mice: a model for detecting antipsychotic activity?

Ouagazzal AM, Jenck F, Moreau JL.

Psychopharmacology (Berl). 2001 Jul;156(2-3):273-83.

PMID:
11549229
32.

Pharmacological characterization of the novel nonpeptide orphanin FQ/nociceptin receptor agonist Ro 64-6198: rapid and reversible desensitization of the ORL1 receptor in vitro and lack of tolerance in vivo.

Dautzenberg FM, Wichmann J, Higelin J, Py-Lang G, Kratzeisen C, Malherbe P, Kilpatrick GJ, Jenck F.

J Pharmacol Exp Ther. 2001 Aug;298(2):812-9.

PMID:
11454946
33.

Influence of the selective ORL1 receptor agonist, Ro64-6198, on rodent neurological function.

Higgins GA, Grottick AJ, Ballard TM, Richards JG, Messer J, Takeshima H, Pauly-Evers M, Jenck F, Adam G, Wichmann J.

Neuropharmacology. 2001 Jul;41(1):97-107.

PMID:
11445190
34.

Effects of Ro 64-6198 in nociceptin/orphanin FQ-sensitive isolated tissues.

Rizzi D, Bigoni R, Rizzi A, Jenck F, Wichmann J, Guerrini R, Regoli D, Calo G.

Naunyn Schmiedebergs Arch Pharmacol. 2001 May;363(5):551-5.

PMID:
11383716
35.

The brain decade in debate: II. Panic or anxiety? From animal models to a neurobiological basis.

Andreatini R, Blanchard C, Blanchard R, Brandão ML, Carobrez AP, Griebel G, Guimarães FS, Handley SL, Jenck F, Leite JR, Rodgers J, Schenberg LC, Da Cunha C, Graeff FG.

Braz J Med Biol Res. 2001 Feb;34(2):145-54. Review.

36.

High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.

Röver S, Adam G, Cesura AM, Galley G, Jenck F, Monsma FJ Jr, Wichmann J, Dautzenberg FM.

J Med Chem. 2000 Apr 6;43(7):1329-38.

PMID:
10753470
37.

OrphaninFQ: role in behavioral fear responses and vulnerability to stress?

Jenck F, Ouagazzal AM, Pauly-Evers M, Moreau JL.

Mol Psychiatry. 2000 Nov;5(6):572-4. No abstract available.

PMID:
11126386
38.

Spatial and associative learning deficits induced by neonatal excitotoxic hippocampal damage in rats: further evaluation of an animal model of schizophrenia.

Le Pen G, Grottick AJ, Higgins GA, Martin JR, Jenck F, Moreau JL.

Behav Pharmacol. 2000 Jun;11(3-4):257-68.

PMID:
11103880
39.
40.

Functional consequences of reduction in NMDA receptor glycine affinity in mice carrying targeted point mutations in the glycine binding site.

Kew JN, Koester A, Moreau JL, Jenck F, Ouagazzal AM, Mutel V, Richards JG, Trube G, Fischer G, Montkowski A, Hundt W, Reinscheid RK, Pauly-Evers M, Kemp JA, Bluethmann H.

J Neurosci. 2000 Jun 1;20(11):4037-49.

41.

ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.

Röver S, Wichmann J, Jenck F, Adam G, Cesura AM.

Bioorg Med Chem Lett. 2000 Apr 17;10(8):831-4.

PMID:
10782696
42.

A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat.

Jenck F, Wichmann J, Dautzenberg FM, Moreau JL, Ouagazzal AM, Martin JR, Lundstrom K, Cesura AM, Poli SM, Roever S, Kolczewski S, Adam G, Kilpatrick G.

Proc Natl Acad Sci U S A. 2000 Apr 25;97(9):4938-43.

43.

8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.

Wichmann J, Adam G, Röver S, Cesura AM, Dautzenberg FM, Jenck F.

Bioorg Med Chem Lett. 1999 Aug 16;9(16):2343-8.

PMID:
10476866
44.

The 5-HT1A receptor agonist flesinoxan increases aversion in a model of panic-like anxiety in rats.

Jenck F, Martin JR, Moreau JL.

J Psychopharmacol. 1999;13(2):166-70.

PMID:
10475723
45.

Targeted disruption of the orphanin FQ/nociceptin gene increases stress susceptibility and impairs stress adaptation in mice.

Köster A, Montkowski A, Schulz S, Stübe EM, Knaudt K, Jenck F, Moreau JL, Nothacker HP, Civelli O, Reinscheid RK.

Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10444-9.

46.

Antiaversive effects of 5HT2C receptor agonists and fluoxetine in a model of panic-like anxiety in rats.

Jenck F, Moreau JL, Berendsen HH, Boes M, Broekkamp CL, Martin JR, Wichmann J, Van Delft AM.

Eur Neuropsychopharmacol. 1998 Aug;8(3):161-8.

PMID:
9716307
47.

5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential.

Martin JR, Bös M, Jenck F, Moreau J, Mutel V, Sleight AJ, Wichmann J, Andrews JS, Berendsen HH, Broekkamp CL, Ruigt GS, Köhler C, Delft AM.

J Pharmacol Exp Ther. 1998 Aug;286(2):913-24.

PMID:
9694950
48.

Sarmazenil-precipitated withdrawal: a reliable method for assessing dependence liability of benzodiazepine receptor ligands.

Martin JR, Moreau JL, Jenck F, Pieri L.

Pharmacol Biochem Behav. 1998 Apr;59(4):939-44.

PMID:
9586852
49.

Orphanin FQ acts as an anxiolytic to attenuate behavioral responses to stress.

Jenck F, Moreau JL, Martin JR, Kilpatrick GJ, Reinscheid RK, Monsma FJ Jr, Nothacker HP, Civelli O.

Proc Natl Acad Sci U S A. 1997 Dec 23;94(26):14854-8.

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