459
Views
39
CrossRef citations to date
0
Altmetric
Review

Bi-phasic dose response in the preclinical and clinical developments of sigma-1 receptor ligands for the treatment of neurodegenerative disorders

ORCID Icon
Pages 373-389 | Received 03 Jun 2020, Accepted 14 Oct 2020, Published online: 27 Oct 2020

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (2)

Shao-Ming Wang, Hsiang-En Wu, Yuko Yasui, Michal Geva, Michael Hayden, Tangui Maurice, Mauro Cozzolino & Tsung-Ping Su. (2023) Nucleoporin POM121 signals TFEB-mediated autophagy via activation of SIGMAR1/sigma-1 receptor chaperone by pridopidine. Autophagy 19:1, pages 126-151.
Read now
Mani Iyer Prasanth, Dicson Sheeja Malar, Tewin Tencomnao & James Michael Brimson. (2021) The emerging role of the sigma-1 receptor in autophagy: hand-in-hand targets for the treatment of Alzheimer’s. Expert Opinion on Therapeutic Targets 25:5, pages 401-414.
Read now

Articles from other publishers (37)

Aline Freyssin, Allison Carles, Sarra Guehairia, Gilles Rubinstenn & Tangui Maurice. (2024) Fluoroethylnormemantine (FENM) shows synergistic protection in combination with a sigma-1 receptor agonist in a mouse model of Alzheimer's disease. Neuropharmacology 242, pages 109733.
Crossref
Lucie Crouzier, Johann Meunier, Allison Carles, Axelle Morilleau, Cassandre Vrigneau, Martine Schmitt, Jean‐Jacques Bourguignon, Benjamin Delprat & Tangui Maurice. (2023) Convolamine, a tropane alkaloid extracted from Convolvulus plauricalis , is a potent sigma‐1 receptor‐positive modulator with cognitive and neuroprotective properties . Phytotherapy Research.
Crossref
Carmen Abate & Tangui Maurice. (2023) The Intriguing Sigma-1 and Sigma-2 Receptors and Their Potential Therapeutic Roles 2.0. International Journal of Molecular Sciences 24:21, pages 15868.
Crossref
Meewhi Kim & Ilya Bezprozvanny. (2023) Structure-Based Modeling of Sigma 1 Receptor Interactions with Ligands and Cholesterol and Implications for Its Biological Function. International Journal of Molecular Sciences 24:16, pages 12980.
Crossref
Katarzyna Szczepańska, Andrzej J. Bojarski, Piotr Popik & Natalia Malikowska-Racia. (2023) Novel object recognition test as an alternative approach to assessing the pharmacological profile of sigma-1 receptor ligands. Pharmacological Reports.
Crossref
Jing Zhao, Rajalakshmi Veeranan-Karmegam, Frederick C. Baker, Barbara A. Mysona, Pritha Bagchi, Yutao Liu, Sylvia B. Smith, Graydon B. Gonsalvez & Kathryn E. Bollinger. (2023) Defining the ligand-dependent proximatome of the sigma 1 receptor. Frontiers in Cell and Developmental Biology 11.
Crossref
Jo Sourbron & Lieven Lagae. (2023) Fenfluramine: a plethora of mechanisms?. Frontiers in Pharmacology 14.
Crossref
Edijs Vavers, Liga Zvejniece & Maija Dambrova. (2023) Sigma-1 receptor and seizures. Pharmacological Research 191, pages 106771.
Crossref
Dicson S. Malar, Premrutai Thitilertdecha, Kanokphorn S. Ruckvongacheep, Sirikalaya Brimson, Tewin Tencomnao & James M. Brimson. (2023) Targeting Sigma Receptors for the Treatment of Neurodegenerative and Neurodevelopmental Disorders. CNS Drugs 37:5, pages 399-440.
Crossref
Borje Darpo, Michal Geva, Georg Ferber, Yigal Paul Goldberg, Andres Cruz-Herranz, Munish Mehra, Richard Kovacs & Michael R. Hayden. (2023) Pridopidine Does Not Significantly Prolong the QTc Interval at the Clinically Relevant Therapeutic Dose. Neurology and Therapy 12:2, pages 597-617.
Crossref
Jing Li, Kenneth A. Satyshur, Lian-Wang Guo & Arnold E. Ruoho. (2023) Sphingoid Bases Regulate the Sigma-1 Receptor—Sphingosine and N,N’-Dimethylsphingosine Are Endogenous Agonists. International Journal of Molecular Sciences 24:4, pages 3103.
Crossref
Agnieszka Piechal, Alicja Jakimiuk, Justyna Pyrzanowska, Kamilla Blecharz-Klin, Ilona Joniec-Maciejak, Alicja Wiercińska-Drapało, Dagmara Mirowska-Guzel & Ewa Widy-Tyszkiewicz. (2023) Long-term Administration of 3-Di-O-Tolylguanidine Modulates Spatial Learning and Memory in Rats and Causes Transition in the Concentration of Neurotransmitters in the Hippocampus, Prefrontal Cortex and Striatum. Neuroscience 510, pages 129-146.
Crossref
Mikhail V. Voronin, Elena V. Abramova, Ekaterina R. Verbovaya, Yulia V. Vakhitova & Sergei B. Seredenin. (2023) Chaperone-Dependent Mechanisms as a Pharmacological Target for Neuroprotection. International Journal of Molecular Sciences 24:1, pages 823.
Crossref
Mengyu Du, Tao Jiang, Shuxuan He, Bo Cheng, Xin Zhang, Liya Li, Lan Yang, Wei Gao, Yansong Li & Qiang Wang. (2023) Sigma-1 Receptor as a Protective Factor for Diabetes-Associated Cognitive Dysfunction via Regulating Astrocytic Endoplasmic Reticulum-Mitochondrion Contact and Endoplasmic Reticulum Stress. Cells 12:1, pages 197.
Crossref
Anum Rasheed, Ahmad Bin Zaheer, Aqsa Munawwar, Zouina Sarfraz, Azza Sarfraz, Karla Robles-Velasco & Ivan Cherrez-Ojeda. (2022) The Allosteric Antagonist of the Sigma-2 Receptors—Elayta (CT1812) as a Therapeutic Candidate for Mild to Moderate Alzheimer’s Disease: A Scoping Systematic Review. Life 13:1, pages 1.
Crossref
Christelle Lasbleiz, Amandine Peyrel, Pauline Tarot, Jérôme Sarniguet, Lucie Crouzier, Nicolas Cubedo, Benjamin Delprat, Mireille Rossel, Tangui Maurice & Jean-Charles Liévens. (2022) Sigma-1 receptor agonist PRE-084 confers protection against TAR DNA-binding protein-43 toxicity through NRF2 signalling. Redox Biology 58, pages 102542.
Crossref
Jingyun Wu, Luisa Möhle, Thomas Brüning, Iván Eiriz, Muhammad Rafehi, Katja Stefan, Sven Marcel Stefan & Jens Pahnke. (2022) A Novel Huntington’s Disease Assessment Platform to Support Future Drug Discovery and Development. International Journal of Molecular Sciences 23:23, pages 14763.
Crossref
Lucas Mele, Raphael El Bekri Saudain, Jean-Luc Pirat, David Virieux & Tahar Ayad. (2022) Efficient microwave-assisted selective alkaline hydrolysis of diversely substituted phosphonate esters. Green Chemistry 24:20, pages 7900-7905.
Crossref
Bénédicte Oxombre, Fahima Madouri, Anne-Sophie Journé, Séverine Ravez, Eloise Woitrain, Pascal Odou, Nathalie Duhal, Sandro Ninni, David Montaigne, Nadira Delhem, Patrick Vermersch & Patricia Melnyk. (2022) Safe and Efficient Sigma1 Ligand: A Potential Drug Candidate for Multiple Sclerosis. International Journal of Molecular Sciences 23:19, pages 11893.
Crossref
Jing Li, Elisa Félix-Soriano, Katherine R. Wright, Hongtao Shen, Lisa A. Baer, Kristin I. Stanford & Lian-Wang Guo. (2022) Differential Responses to Sigma-1 or Sigma-2 Receptor Ablation in Adiposity, Fat Oxidation, and Sexual Dimorphism. International Journal of Molecular Sciences 23:18, pages 10846.
Crossref
Kenji Mishiro, Mengfei Wang, Saki Hirata, Takeshi Fuchigami, Kazuhiro Shiba, Seigo Kinuya & Kazuma Ogawa. (2022) Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics. RSC Medicinal Chemistry 13:8, pages 986-997.
Crossref
Núria Gaja-Capdevila, Neus Hernández, Sandra Yeste, Raquel F. Reinoso, Javier Burgueño, Ana Montero, Manuel Merlos, José M. Vela, Mireia Herrando-Grabulosa & Xavier Navarro. (2022) EST79232 and EST79376, Two Novel Sigma-1 Receptor Ligands, Exert Neuroprotection on Models of Motoneuron Degeneration. International Journal of Molecular Sciences 23:12, pages 6737.
Crossref
Peng Ren, Jingya Wang, Nanxi Li, Guangxiang Li, Hui Ma, Yongqi Zhao & Yunfeng Li. (2022) Sigma-1 Receptors in Depression: Mechanism and Therapeutic Development. Frontiers in Pharmacology 13.
Crossref
Patrick Cottilli, Núria Gaja-Capdevila & Xavier Navarro. (2022) Effects of Sigma-1 Receptor Ligands on Peripheral Nerve Regeneration. Cells 11:7, pages 1083.
Crossref
Emőke Borbély, Viktória Varga, Titanilla Szögi, Ildikó Schuster, Zsolt Bozsó, Botond Penke & Lívia Fülöp. (2022) Impact of Two Neuronal Sigma-1 Receptor Modulators, PRE084 and DMT, on Neurogenesis and Neuroinflammation in an Aβ1–42-Injected, Wild-Type Mouse Model of AD. International Journal of Molecular Sciences 23:5, pages 2514.
Crossref
Lucie Crouzier, Alberto Danese, Yuko YasuiElodie M. Richard, Jean-Charles Liévens, Simone Patergnani, Simon CoulyCamille DiezMorgane DenusNicolas CubedoMireille Rossel, Marc Thiry, Tsung-Ping Su, Paolo PintonTangui Maurice & Benjamin Delprat. (2022) Activation of the sigma-1 receptor chaperone alleviates symptoms of Wolfram syndrome in preclinical models. Science Translational Medicine 14:631.
Crossref
Parthena Martin, Tangui Maurice, Arnold Gammaitoni, Gail Farfel, Brooks Boyd & Bradley Galer. (2022) Fenfluramine modulates the anti-amnesic effects induced by sigma-1 receptor agonists and neuro(active)steroids in vivo. Epilepsy & Behavior 127, pages 108526.
Crossref
Francesca S. Abatematteo, Philip D. Mosier, Mauro Niso, Leonardo Brunetti, Francesco Berardi, Fulvio Loiodice, Marialessandra Contino, Benjamin Delprat, Tangui Maurice, Antonio Laghezza & Carmen Abate. (2022) Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ1) receptor ligands with potent anti-amnesic effect. European Journal of Medicinal Chemistry 228, pages 114038.
Crossref
Michal Geva, Noga Gershoni-Emek, Luana Naia, Philip Ly, Sandra Mota, Ana Cristina Rego, Michael R. Hayden & Leonard A. Levin. (2021) Neuroprotection of retinal ganglion cells by the sigma-1 receptor agonist pridopidine in models of experimental glaucoma. Scientific Reports 11:1.
Crossref
Lucie Crouzier, Morgane Denus, Elodie M. Richard, Amarande Tavernier, Camille Diez, Nicolas Cubedo, Tangui Maurice & Benjamin Delprat. (2021) Sigma-1 Receptor Is Critical for Mitochondrial Activity and Unfolded Protein Response in Larval Zebrafish. International Journal of Molecular Sciences 22:20, pages 11049.
Crossref
Parthena Martin, Thadd Reeder, Jo Sourbron, Peter A. M. de Witte, Arnold R. Gammaitoni & Bradley S. Galer. (2021) An Emerging Role for Sigma-1 Receptors in the Treatment of Developmental and Epileptic Encephalopathies. International Journal of Molecular Sciences 22:16, pages 8416.
Crossref
Mikhail V. Voronin, Yulia V. Vakhitova, Inna P. Tsypysheva, Dmitry O. Tsypyshev, Inna V. Rybina, Rustam D. Kurbanov, Elena V. Abramova & Sergei B. Seredenin. (2021) Involvement of Chaperone Sigma1R in the Anxiolytic Effect of Fabomotizole. International Journal of Molecular Sciences 22:11, pages 5455.
Crossref
Rareş-Petru Moldovan, Daniel Gündel, Rodrigo Teodoro, Friedrich-Alexander Ludwig, Steffen Fischer, Magali Toussaint, Dirk Schepmann, Bernhard Wünsch, Peter Brust & Winnie Deuther-Conrad. (2021) Design, Radiosynthesis and Preliminary Biological Evaluation in Mice of a Brain-Penetrant 18F-Labelled σ2 Receptor Ligand. International Journal of Molecular Sciences 22:11, pages 5447.
Crossref
Shujun Chen, Tianyu Liang, Tao Xue, Shouru Xue & Qun Xue. (2021) Pridopidine for the Improvement of Motor Function in Patients With Huntington's Disease: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Frontiers in Neurology 12.
Crossref
Vladimir Zhemkov, Michal Geva, Michael R. Hayden & Ilya Bezprozvanny. (2021) Sigma-1 Receptor (S1R) Interaction with Cholesterol: Mechanisms of S1R Activation and Its Role in Neurodegenerative Diseases. International Journal of Molecular Sciences 22:8, pages 4082.
Crossref
Luana Naia, Philip Ly, Sandra I. Mota, Carla Lopes, Carina Maranga, Patrícia Coelho, Noga Gershoni-Emek, Maria Ankarcrona, Michal Geva, Michael R. Hayden & A. Cristina Rego. (2021) The Sigma-1 Receptor Mediates Pridopidine Rescue of Mitochondrial Function in Huntington Disease Models. Neurotherapeutics 18:2, pages 1017-1038.
Crossref
Kenji Hashimoto. (2021) Repurposing of CNS drugs to treat COVID-19 infection: targeting the sigma-1 receptor. European Archives of Psychiatry and Clinical Neuroscience 271:2, pages 249-258.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.