Literature DB >> 23589487

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

Michel A Steiner1, John Gatfield, Catherine Brisbare-Roch, Hendrik Dietrich, Alexander Treiber, Francois Jenck, Christoph Boss.   

Abstract

Stress relief: Orexin neuropeptides regulate arousal and stress processing through orexin receptor type 1 (OXR-1) and 2 (OXR-2) signaling. A selective OXR-1 antagonist, represented by a phenylglycine-amide substituted tetrahydropapaverine derivative (ACT-335827), is described that is orally available, penetrates the brain, and decreases fear, compulsive behaviors and autonomic stress reactions in rats.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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Year:  2013        PMID： 23589487     DOI： 10.1002/cmdc.201300003

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  30 in total

1.  Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor.

Authors:  David A Perrey; Nadezhda A German; Ann M Decker; David Thorn; Jun-Xu Li; Brian P Gilmour; Brian F Thomas; Danni L Harris; Scott P Runyon; Yanan Zhang
Journal:  ACS Chem Neurosci       Date:  2015-02-12       Impact factor: 4.418

2.  Hypocretin receptor 1 blockade preferentially reduces high effort responding for cocaine without promoting sleep.

Authors:  Zachary D Brodnik; David L Bernstein; Courtney D Prince; Rodrigo A España
Journal:  Behav Brain Res       Date:  2015-06-03       Impact factor: 3.332

3.  Structure-based development of a subtype-selective orexin 1 receptor antagonist.

Authors:  Jan Hellmann; Matthäus Drabek; Jie Yin; Jakub Gunera; Theresa Pröll; Frank Kraus; Christopher J Langmead; Harald Hübner; Dorothee Weikert; Peter Kolb; Daniel M Rosenbaum; Peter Gmeiner
Journal:  Proc Natl Acad Sci U S A       Date:  2020-07-15       Impact factor: 11.205

Review 4.  Orexin/hypocretin based pharmacotherapies for the treatment of addiction: DORA or SORA?

Authors:  Shaun Yon-Seng Khoo; Robyn Mary Brown
Journal:  CNS Drugs       Date:  2014-08       Impact factor: 5.749

5.  A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects.

Authors:  Pascal Bonaventure; Sujin Yun; Philip L Johnson; Anantha Shekhar; Stephanie D Fitz; Brock T Shireman; Terry P Lebold; Diane Nepomuceno; Brian Lord; Michelle Wennerholm; Jonathan Shelton; Nicholas Carruthers; Timothy Lovenberg; Christine Dugovic
Journal:  J Pharmacol Exp Ther       Date:  2015-01-12       Impact factor: 4.030

6.  An alerting structure: human orexin receptor 1.

Authors:  Daniel Wacker; Bryan L Roth
Journal:  Nat Struct Mol Biol       Date:  2016-04       Impact factor: 15.369

7.  Synthesis and Evaluation of Orexin-1 Receptor Antagonists with Improved Solubility and CNS Permeability.

Authors:  David A Perrey; Ann M Decker; Yanan Zhang
Journal:  ACS Chem Neurosci       Date:  2017-11-20       Impact factor: 4.418

8.  First-in-human study with ACT-539313, a novel selective orexin-1 receptor antagonist.

Authors:  Priska Kaufmann; Marion Ort; Georg Golor; Rüdiger Kornberger; Jasper Dingemanse
Journal:  Br J Clin Pharmacol       Date:  2020-03-06       Impact factor: 4.335

Review 9.  Intranasal administration of orexin peptides: Mechanisms and therapeutic potential for age-related cognitive dysfunction.

Authors:  Coleman B Calva; Jim R Fadel
Journal:  Brain Res       Date:  2018-08-24       Impact factor: 3.252

Review 10.  Therapeutics development for addiction: Orexin-1 receptor antagonists.

Authors:  David A Perrey; Yanan Zhang
Journal:  Brain Res       Date:  2018-08-24       Impact factor: 3.252
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