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Alexander Treiber

Explore the profile of Alexander Treiber including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 48
Citations 564
Followers 0
Related Specialties
Pharmacology
Biochemistry
Chemistry
Top 10 Co-Authors
Christoph Boss
John Gatfield
Martin H Bolli
Patrick Hess
Thierry Sifferlen
Swen Seeland
Jodi T Williams
Christine Brotschi
Francois Jenck
Stephane Delahaye
Published In
Xenobiotica
Bioorg Med Chem Lett
J Med Chem
ChemMedChem
J Pharmacol Exp Ther
Affiliations
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Recent Articles
21.
ATP-induced cellular stress and mitochondrial toxicity in cells expressing purinergic P2X7 receptor
Seeland S, Kettiger H, Murphy M, Treiber A, Giller J, Kiss A, et al.
Pharmacol Res Perspect . 2015 Jun; 3(2):e00123. PMID: 26038699
Under pathological conditions, the purinergic P2X7 receptor is activated by elevated concentrations of extracellular ATP. Thereby, the receptor forms a slowly dilating pore, allowing cations and, upon prolonged stimulation, large...
22.
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, et al.
Bioorg Med Chem Lett . 2015 Apr; 25(9):1884-91. PMID: 25838147
Starting from advanced pyrrolidin-2-one lead compounds, this novel series of small-molecule orexin receptor antagonists was further optimized by fine-tuning of the C-3 substitution at the γ-lactam ring. We discuss our...
23.
Pharmacokinetic interactions between simvastatin and setipiprant, a CRTH2 antagonist
Gehin M, Sidharta P, Gnerre C, Treiber A, Halabi A, Dingemanse J
Eur J Clin Pharmacol . 2014 Oct; 71(1):15-23. PMID: 25323804
Purpose: Setipiprant, a selective oral CRTH2 antagonist, has been investigated for the treatment of allergic rhinitis and asthma. In vitro data showed that setipiprant has a weak induction potential on...
24.
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 M, Treiber A, Dietrich H, Jenck F, et al.
ChemMedChem . 2014 Aug; 9(11):2486-96. PMID: 25147058
The orexin system consists of two G-protein-coupled receptors, the orexin 1 and orexin 2 receptors, widely expressed in diverse regions of the brain, and two peptide agonists, orexin A and...
25.
Optimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y(12) antagonists for inhibition of platelet aggregation
Caroff E, Meyer E, Treiber A, Hilpert K, Riederer M
Bioorg Med Chem Lett . 2014 Aug; 24(17):4323-31. PMID: 25113932
2-Phenyl-pyrimidine-4-carboxamide analogs were identified as P2Y12 antagonists. Optimization of the carbon-linked or nitrogen-linked substituent at the 6-position of the pyrimidine ring provided compounds with excellent ex vivo potency in the...
26.
Macitentan does not interfere with hepatic bile salt transport
Treiber A, Aanismaa P, de Kanter R, Delahaye S, Treher M, Hess P, et al.
J Pharmacol Exp Ther . 2014 Apr; 350(1):130-43. PMID: 24769543
Treatment of pulmonary arterial hypertension with the endothelin receptor antagonist bosentan has been associated with transient increases in liver transaminases. Mechanistically, bosentan inhibits the bile salt export pump (BSEP) leading...
27.
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, et al.
Bioorg Med Chem Lett . 2014 Jan; 24(4):1201-8. PMID: 24447850
Starting from a thiazolidin-4-one HTS hit, a novel series of substituted lactams was identified and developed as dual orexin receptor antagonists. In this Letter, we describe our initial efforts towards...
28.
Novel S1P1 receptor agonists--part 1: From pyrazoles to thiophenes
Bolli M, Muller C, Mathys B, Abele S, Birker M, Bravo R, et al.
J Med Chem . 2013 Nov; 56(23):9737-55. PMID: 24266709
From a high-throughput screening campaign aiming at the identification of novel S1P1 receptor agonists, the pyrazole derivative 2 emerged as a hit structure. Medicinal chemistry efforts focused not only on...
29.
Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist
Steiner M, Gatfield J, Brisbare-Roch C, Dietrich H, Treiber A, Jenck F, et al.
ChemMedChem . 2013 Apr; 8(6):898-903. PMID: 23589487
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...
30.
Elucidation of the metabolic pathways and the resulting multiple metabolites of almorexant, a dual orexin receptor antagonist, in humans
Dingemanse J, Hoever P, Hoch M, Treiber A, Wagner-Redeker W, Miraval T, et al.
Drug Metab Dispos . 2013 Feb; 41(5):1046-59. PMID: 23431113
Almorexant [(2R)-2-{(1S)-6, 7-dimethoxy-1-[2-(4-trifluoromethyl-phenyl)-ethyl]-3,4-dihydro-1H-isoquinolin-2-yl}-N-methyl-2-phenyl-acetamide], a tetrahydroisoquinoline derivative, is a dual orexin receptor antagonist with sleep-promoting properties in both animals and humans. This study investigated the disposition, metabolism, and elimination of almorexant...