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Items: 1 to 20 of 137

1.

Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds.

Temme L, Bechthold E, Schreiber JA, Gawaskar S, Schepmann D, Robaa D, Sippl W, Seebohm G, Wünsch B.

Eur J Med Chem. 2020 Feb 10;190:112138. doi: 10.1016/j.ejmech.2020.112138. [Epub ahead of print]

PMID:
32070917
2.

Design and synthesis of N‑(benzylpiperidinyl)‑4‑fluorobenzamide: A haloperidol analog that reduces neuropathic nociception via σ1 receptor antagonism.

Déciga-Campos M, Melo-Hernández LA, Torres-Gómez H, Wünsch B, Schepmann D, González-Trujano ME, Espinosa-Juárez J, López-Muñoz FJ, Navarrete-Vázquez G.

Life Sci. 2020 Jan 23;245:117348. doi: 10.1016/j.lfs.2020.117348. [Epub ahead of print]

PMID:
31981633
3.

Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines.

Baumeister S, Schepmann D, Wünsch B.

Bioorg Med Chem. 2020 Jan 15;28(2):115245. doi: 10.1016/j.bmc.2019.115245. Epub 2019 Dec 9.

PMID:
31843460
4.

New Insights into the Opening of the Occluded Ligand-Binding Pocket of Sigma1 Receptor: Binding of a Novel Bivalent RC-33 Derivative.

Rossino G, Orellana I, Caballero J, Schepmann D, Wünsch B, Rui M, Rossi D, González-Avendaño M, Collina S, Vergara-Jaque A.

J Chem Inf Model. 2020 Feb 24;60(2):756-765. doi: 10.1021/acs.jcim.9b00649. Epub 2019 Dec 20.

PMID:
31809025
5.

A common mechanism allows selective targeting of GluN2B subunit-containing N-methyl-D-aspartate receptors.

Schreiber JA, Schepmann D, Frehland B, Thum S, Datunashvili M, Budde T, Hollmann M, Strutz-Seebohm N, Wünsch B, Seebohm G.

Commun Biol. 2019 Nov 15;2:420. doi: 10.1038/s42003-019-0645-6. eCollection 2019.

6.

Pharmacological characterization of high-affinity σ1 receptor ligands with spirocyclic thienopyran and thienofuran scaffold.

Schepmann D, Neue C, Westphälinger S, Müller C, Bracher F, Lange C, Bednarski P, Almansa C, Friedland K, Räbiger V, Düfer M, Wünsch B.

J Pharm Pharmacol. 2020 Feb;72(2):236-248. doi: 10.1111/jphp.13196. Epub 2019 Nov 19.

PMID:
31743446
7.

Structure-Affinity Relationships of 2,3,4,5-Tetrahydro-1H-3-benzazepine and 6,7,8,9-Tetrahydro-5H-benzo[7]annulen-7-amine Analogues and the Discovery of a Radiofluorinated 2,3,4,5-Tetrahydro-1H-3-benzazepine Congener for Imaging GluN2B Subunit-Containing N-Methyl-d-aspartate Receptors.

Ahmed H, Haider A, Varisco J, Stanković M, Wallimann R, Gruber S, Iten I, Häne S, Müller Herde A, Keller C, Schibli R, Schepmann D, Mu L, Wünsch B, Ametamey SM.

J Med Chem. 2019 Nov 14;62(21):9450-9470. doi: 10.1021/acs.jmedchem.9b00812. Epub 2019 Oct 28.

PMID:
31657559
8.

Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation.

Temme L, Börgel F, Schepmann D, Robaa D, Sippl W, Daniliuc C, Wünsch B.

Bioorg Med Chem. 2019 Dec 1;27(23):115146. doi: 10.1016/j.bmc.2019.115146. Epub 2019 Oct 8.

PMID:
31648876
9.

Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.

Zampieri D, Fortuna S, Calabretti A, Romano M, Menegazzi R, Schepmann D, Wünsch B, Collina S, Zanon D, Mamolo MG.

Eur J Med Chem. 2019 Oct 15;180:268-282. doi: 10.1016/j.ejmech.2019.07.012. Epub 2019 Jul 8.

PMID:
31319263
10.

Investigation of the Role of Chirality in the Interaction with σ Receptors and Effect on Binge Eating Episode of a Potent σ1 Antagonist Analogue of Spipethiane.

Del Bello F, Micioni Di Bonaventura MV, Bonifazi A, Wünsch B, Schepmann D, Giancola JB, Micioni Di Bonaventura E, Vistoli G, Giorgioni G, Quaglia W, Piergentili A, Cifani C.

ACS Chem Neurosci. 2019 Aug 21;10(8):3391-3397. doi: 10.1021/acschemneuro.9b00261. Epub 2019 Jul 23.

PMID:
31298830
11.

In vitro and in vivo Human Metabolism of (S)-[18F]Fluspidine - A Radioligand for Imaging σ1 Receptors With Positron Emission Tomography (PET).

Ludwig FA, Fischer S, Houska R, Hoepping A, Deuther-Conrad W, Schepmann D, Patt M, Meyer PM, Hesse S, Becker GA, Zientek FR, Steinbach J, Wünsch B, Sabri O, Brust P.

Front Pharmacol. 2019 Jun 13;10:534. doi: 10.3389/fphar.2019.00534. eCollection 2019.

12.

Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.

Wagner M, Schepmann D, Ametamey SM, Wünsch B.

Bioorg Med Chem. 2019 Aug 15;27(16):3559-3567. doi: 10.1016/j.bmc.2019.06.035. Epub 2019 Jun 20.

PMID:
31255496
13.

Structure-Affinity Relationships of Fluorinated Spirocyclic σ2 Receptor Ligands with an Exocyclic Benzylamino Moiety.

Bergkemper M, Kronenberg E, Schepmann D, Ludwig FA, Brust P, Wünsch B.

ChemMedChem. 2019 Aug 6;14(15):1392-1402. doi: 10.1002/cmdc.201900284. Epub 2019 Jul 12.

PMID:
31189022
14.

Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and σ1 receptor antagonists: Synthesis, receptor affinity, selectivity and antiallodynic activity.

Thum S, Schepmann D, Ayet E, Pujol M, Nieto FR, Ametamey SM, Wünsch B.

Eur J Med Chem. 2019 Sep 1;177:47-62. doi: 10.1016/j.ejmech.2019.05.034. Epub 2019 May 16.

PMID:
31129453
15.

Pharmacokinetic properties of enantiomerically pure GluN2B selective NMDA receptor antagonists with 3-benzazepine scaffold.

Börgel F, Galla F, Lehmkuhl K, Schepmann D, Ametamey SM, Wünsch B.

J Pharm Biomed Anal. 2019 Aug 5;172:214-222. doi: 10.1016/j.jpba.2019.04.032. Epub 2019 Apr 16.

PMID:
31060034
16.

Role of the NMDA Receptor in the Antitumor Activity of Chiral 1,4-Dioxane Ligands in MCF-7 and SKBR3 Breast Cancer Cells.

Morelli MB, Amantini C, Nabissi M, Santoni G, Wünsch B, Schepmann D, Cimarelli C, Pellei M, Santini C, Fontana S, Mammoli V, Quaglia W, Bonifazi A, Giannella M, Giorgioni G, Piergentili A, Del Bello F.

ACS Med Chem Lett. 2019 Jan 28;10(4):511-516. doi: 10.1021/acsmedchemlett.8b00536. eCollection 2019 Apr 11.

PMID:
30996788
17.

Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.

Kronenberg E, Weber F, Brune S, Schepmann D, Almansa C, Friedland K, Laurini E, Pricl S, Wünsch B.

J Med Chem. 2019 Apr 25;62(8):4204-4217. doi: 10.1021/acs.jmedchem.9b00449. Epub 2019 Apr 12.

PMID:
30939014
18.

Synthesis and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold.

Baumeister S, Schepmann D, Wünsch B.

Medchemcomm. 2019 Jan 10;10(2):315-325. doi: 10.1039/c8md00545a. eCollection 2019 Feb 1.

19.

Synthesis and pharmacological evaluation of fluorinated benzo[7]annulen-7-amines as GluN2B-selective NMDA receptor antagonists.

Thum S, Schepmann D, Reinoso RF, Alvarez I, Ametamey SM, Wünsch B.

J Labelled Comp Radiopharm. 2019 Jun 30;62(8):354-379. doi: 10.1002/jlcr.3718.

PMID:
30850991
20.

Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.

Tangherlini G, Kalinin DV, Schepmann D, Che T, Mykicki N, Ständer S, Loser K, Wünsch B.

J Med Chem. 2019 Jan 24;62(2):893-907. doi: 10.1021/acs.jmedchem.8b01609. Epub 2019 Jan 9.

PMID:
30543421

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