Journal ArticleDOI
Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
Daniele Zampieri,Erik Laurini,Luciano Vio,Maurizio Fermeglia,Sabrina Pricl,Bernhard Wünsch,Dirk Schepmann,Maria Grazia Mamolo +7 more
TLDR
The design, synthesis, binding evaluation and binding evaluation against σ1 and σ2 receptors of a series of new piperidine-4-carboxamide derivatives variously substituted on the amide nitrogen atom are reported.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2015-01-27. It has received 18 citations till now. The article focuses on the topics: Piperidine & Carboxamide.read more
Citations
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Journal ArticleDOI
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
TL;DR: This review provides up-to-date information on the selective targeting of σ1 receptors, including their history, function, reported crystal structures, and roles in neurological diseases, as well as a useful collation of new chemical entities as ρ1 selective orthosteric ligands or allosteric modulators.
Journal ArticleDOI
Synthesis, cytotoxicity and antiviral evaluation of new series of imidazo[4,5-g]quinoline and pyrido[2,3-g]quinoxalinone derivatives
Irene Briguglio,Roberta Loddo,Erik Laurini,Maurizio Fermeglia,Sandra Piras,Paola Corona,Paolo Giunchedi,Elisabetta Gavini,Giuseppina Sanna,Gabriele Giliberti,Cristina Ibba,Pamela Farci,Paolo La Colla,Sabrina Pricl,Antonio Carta +14 more
TL;DR: Following the research program on new antiviral agents, the pyrido[2,3-g]quinoxalinone nucleus was found endowed with high potency against several pathogenic RNA viruses as etiological agents of important veterinary and human pathologies and molecular simulation results provided a molecular rationale for the anti-BVDV activity.
Journal ArticleDOI
Neuroprotection in non-transgenic and transgenic mouse models of Alzheimer's disease by positive modulation of σ1 receptors.
Tangui Maurice,Jean-Noël Volle,Manon Strehaiano,Lucie Crouzier,Claire Pereira,Nikolay Kaloyanov,David Virieux,Jean-Luc Pirat +7 more
TL;DR: This study shows that σ1 PM with high neuropotective potential can be identified, combining pharmacological efficacy, selectivity and therapeutic safety, and identifies a novel promising compound, OZP002.
Journal ArticleDOI
New neurogenic lipoic-based hybrids as innovative Alzheimer's drugs with σ-1 agonism and β-secretase inhibition.
Martín Estrada,Concepción Pérez,Elena Soriano,Erik Laurini,Maurizio Romano,Sabrina Pricl,José A. Morales-García,Ana Perez-Castillo,María Isabel Rodríguez-Franco +8 more
TL;DR: New lipoic-based σ1 agonists endowed with neurogenic, antioxidant, cholinergic and amyloid β-peptide-reducing properties have been discovered for the potential treatment of AD.
Journal ArticleDOI
Rigidity versus Flexibility: Is This an Issue in σ1 Receptor Ligand Affinity and Activity?
Frauke Weber,Stefanie Brune,Frederik Börgel,Carsten Lange,Katharina Korpis,Patrick J. Bednarski,Erik Laurini,Maurizio Fermeglia,Sabrina Pricl,Dirk Schepmann,Bernhard Wünsch +10 more
TL;DR: In an in vitro antitumor assay with seven human tumor cell lines, the bicyclic compounds inhibited selectively the growth of the cell line A427, which is due to induction of apoptosis, in this assay, the compounds behave like the known σ1 receptor antagonist haloperidol.
References
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A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
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TL;DR: In this article, the authors compared the Bernal Fowler (BF), SPC, ST2, TIPS2, TIP3P, and TIP4P potential functions for liquid water in the NPT ensemble at 25°C and 1 atm.
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AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility
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TL;DR: AutoDock4 incorporates limited flexibility in the receptor and its utility in analysis of covalently bound ligands is reported, using both a grid‐based docking method and a modification of the flexible sidechain technique.
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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
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The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
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Sigma-1 Receptor Chaperones at the ER- Mitochondrion Interface Regulate Ca2+ Signaling and Cell Survival
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