ArticleNaunyn-Schmiedeberg's archives of pharmacology2004
Antiproliferative and cytotoxic effects of some sigma2 agonists and sigma1 antagonists in tumour cell lines.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
25 citing papers in PubMed.
- Sigma-1 Receptor Ligands for CNS Cancer Treatment.CNS drugs · 2025Review
- Dopamine Partial Agonists in Pregnancy and Lactation: A Systematic Review.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Cytotoxic pathways activated by multifunctional thiosemicarbazones targeting sigma-2 receptors in breast and lung carcinoma cells.Pharmacological reports : PR · 2023Article
- Review
- Sigma-2 Receptor Ligand Binding Modulates Association between TSPO and TMEM97.International journal of molecular sciences · 2023Article
- Biophysical Evaluation and In Vitro Controlled Release of Two Isomeric Adamantane Phenylalkylamines with Antiproliferative/Anticancer and Analgesic Activity.Molecules (Basel, Switzerland) · 2021Article
- Recent Advances in the Development of Sigma Receptor Ligands as Cytotoxic Agents: A Medicinal Chemistry Perspective.Journal of medicinal chemistry · 2021Review
- Combination of Heme Oxygenase-1 Inhibition and Sigma Receptor Modulation for Anticancer Activity.Molecules (Basel, Switzerland) · 2021Article
- Mitochondrial Membranes of Human SH-SY5Y Neuroblastoma Cells Express Serotonin 5-HTInternational journal of molecular sciences · 2020Article
- Sigma-2 Receptor-A Potential Target for Cancer/Alzheimer's Disease Treatment via Its Regulation of Cholesterol Homeostasis.Molecules (Basel, Switzerland) · 2020Review
- Why PB28 Could Be a Covid 2019 Game Changer?ACS medicinal chemistry letters · 2020Article
- Sigma-1 Receptor Positron Emission Tomography: A New Molecular Imaging Approach Using (Molecules (Basel, Switzerland) · 2020Article
- PB28, the Sigma-1 and Sigma-2 Receptors Modulator With Potent Anti-SARS-CoV-2 Activity: A Review About Its Pharmacological Properties and Structure Affinity Relationships.Frontiers in pharmacology · 2020Review
- Small-Molecule Modulators of Sigma1 and Sigma2/TMEM97 in the Context of Cancer: Foundational Concepts and Emerging Themes.Frontiers in pharmacology · 2019Review
- Bridging from Brain to Tumor Imaging: (S)-(-)- and (R)-(+)-[Molecules (Basel, Switzerland) · 2018Article
- Multifunctional thiosemicarbazones and deconstructed analogues as a strategy to study the involvement of metal chelation, Sigma-2 (σEuropean journal of medicinal chemistry · 2018Article
- Article
- Sigma Receptor (σR) Ligands with Antiproliferative and Anticancer Activity.Molecules (Basel, Switzerland) · 2017Review
- Identification of the gene that codes for the σProceedings of the National Academy of Sciences of the United States of America · 2017Article
- Article
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
To establish the activity of sigma ligands at sigma1 and sigma2 receptor, we chose two tumour cell lines, the human SK-N-SH neuroblastoma and the rat C6 glioma lines, which express sigma2 receptors at a high density and sigma1 receptors in their high-affinity or low-affinity state. We tested the sigma2 receptor agonist PB28 and the sigma2 antagonist AC927, and (+)-pentazocine and NE100 as agonist and antagonist, respectively, at sigma1 receptors, with regard to antiproliferative and cytotoxic effects. In addition, 1,3-di(2-tolyl)guanidine (DTG) and haloperidol were tested as reference compounds displaying nearly equipotent sigma affinity (sigma2>sigma1 and sigma1>sigma2, respectively). In both SK-N-SH and C6 cells, PB28 and NE100 displayed the most potent results both in antiproliferative and cytotoxic assay while AC927 and (+)-pentazocine were inactive in both assays. The cytotoxic and antiproliferative effects of DTG and haloperidol reflected their sigma1 antagonist activity and sigma2 agonist activity. Moreover, our results in the tumour cell lines correlated well with those for sigma2 activity found previously in a functional assay in the guinea-pig bladder. These findings establish a new model for evaluating both sigma2 and sigma1 receptor activity of sigma ligands, which could be useful for developing new ligands having mixed sigma2 agonist/sigma1 antagonist activity as potential antineoplastic agents.
Indexed as
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.