ArticleBrain research2012
Neuroprotective effects of high affinity Σ1 receptor selective compounds.
Article in Brain research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.
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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 1 synthesis or guideline pooled it, 34 citations in OpenAlex.
- A neuroprotective target in the shadows: a scoping review of pharmacological gaps in σ1R agonists for glutamate-induced neurotoxicity.Frontiers in pharmacology · 2026Pooled it
- Machine Learning-Driven Discovery of Indole/Oxoindole-Piperazine Scaffolds as Dual MAO-B/Sig-1R Ligands for Neurodegenerative Disorders.Journal of chemical information and modeling · 2026Article
- Sigma‑2 Receptor/Transmembrane Protein 97 in Pain Modulation: Tracing Historical Roots and Current Research Directions.ACS pharmacology & translational science · 2025Review
- Sigma-1 receptor targeting inhibits connexin 43 based intercellular communication in chronic neuropathic pain.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2024Article
- Article
- In vitro characterization of [European journal of pharmacology · 2021Article
- New tetrahydroisoquinoline-based DBioorganic & medicinal chemistry letters · 2021Article
- The Antipsychotic D2AAK1 as a Memory Enhancer for Treatment of Mental and Neurodegenerative Diseases.International journal of molecular sciences · 2020Article
- Dysregulation of Corticostriatal Connectivity in Huntington's Disease: A Role for Dopamine Modulation.Journal of Huntington's disease · 2016Review
- Contribution of Sigma-1 receptor to cytoprotective effect of afobazole.Pharmacology research & perspectives · 2016Article
- The effects of sigma (σ1) receptor-selective ligands on muscarinic receptor antagonist-induced cognitive deficits in mice.British journal of pharmacology · 2015Article
- Roles of sigma-1 receptors in Alzheimer's disease.International journal of clinical and experimental medicine · 2015Review
- Radiosynthesis andMedChemComm · 2014Article
- A possibly sigma-1 receptor mediated role of dimethyltryptamine in tissue protection, regeneration, and immunity.Journal of neural transmission (Vienna, Austria : 1996) · 2013Review
- Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent.EJNMMI research · 2012Article
- Brain-derived neurotrophic factor for high-throughput evaluation of selective Sigma-1 receptor ligands.Journal of pharmacological and toxicological methodsArticle
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
Abstract
We previously reported that the antipsychotic drug haloperidol, a multifunctional D2-like dopamine and sigma receptor subtype antagonist, has neuroprotective properties. In this study we further examined the association between neuroprotection and receptor antagonism by evaluating a panel of novel compounds with varying affinity at sigma and D2-like dopamine receptors. These compounds were evaluated using an in vitro cytotoxicity assay that utilizes a hippocampal-derived cell line, HT-22, in the presence or absence of varying concentrations (5 to 20 mM) of glutamate. While haloperidol was found to be a potent neuroprotective agent in this in vitro cell assay, the prototypic sigma 1 receptor agonist (+)-pentazocine was found not to be neuroprotective. Subsequently, the potency for the neuroprotection of HT-22 cells was evaluated for a) three SV series indoles which have nMolar affinity at D2-like receptors but varying affinity at sigma 1 receptor and b) two benzyl phenylacetamides sigma 1 receptor selective compounds which bind with low affinity at D2-like receptors but have nMolar affinity for the sigma 1 receptor. We observed that cytoprotection correlated with the affinity of the compounds for sigma 1 receptors. Based upon results from the HT-22 cell-based in vitro assay, two phenylacetamides, LS-127 and LS-137, were further evaluated in vivo using a transient middle cerebral artery occlusion (t-MCAO) model of stroke. At a dose of 100 μg/kg, both LS-127 and LS-137 attenuated infarct volume by approximately 50%. These studies provide further evidence that sigma 1 receptor selective compounds can provide neuroprotection in cytotoxic situations. These results also demonstrate that sigma 1 receptor selective benzyl phenylacetamides are candidate pharmacotherapeutic agents that could be used to minimize neuronal death after a stroke or head trauma.
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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.