ArticleInternational journal of molecular sciences2016
TSPO PIGA Ligands Promote Neurosteroidogenesis and Human Astrocyte Well-Being.
Article in International journal of molecular sciences, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 41 citations in OpenAlex.
- Article
- Characteristics of TSPO expression in marmoset EAE.Journal of neuroinflammation · 2025Article
- 18 kDa TSPO targeting drives polarized human microglia towards a protective and restorative neurosteroidome profile.Cellular and molecular life sciences : CMLS · 2025Article
- Indole-Based Compounds in the Development of Anti-Neurodegenerative Agents.Molecules (Basel, Switzerland) · 2024Review
- Chronic administration of XBD173 ameliorates cognitive deficits and neuropathology via 18 kDa translocator protein (TSPO) in a mouse model of Alzheimer's disease.Translational psychiatry · 2023Article
- Indol-3-ylglyoxylamide as Privileged Scaffold in Medicinal Chemistry.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Translocator protein in the rise and fall of central nervous system neurons.Frontiers in cellular neuroscience · 2023Review
- Targeting TSPO Reduces Inflammation and Apoptosis in an In Vitro Photoreceptor-Like Model of Retinal Degeneration.ACS chemical neuroscience · 2022Article
- Translocator Protein Ligand PIGA1138 Reduces Disease Symptoms and Severity in Experimental Autoimmune Encephalomyelitis Model of Primary Progressive Multiple Sclerosis.Molecular neurobiology · 2022Article
- Carbonic anhydrase activation profile of indole-based derivatives.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- TSPO ligand FGIN-1-27 controls priapism in sickle cell mice via endogenous testosterone production.Journal of cellular physiology · 2021Article
- De novo Neurosteroidogenesis in Human Microglia: Involvement of the 18 kDa Translocator Protein.International journal of molecular sciences · 2021Article
- Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets.Molecules (Basel, Switzerland) · 2020Review
- Review
- Mitochondria modulatory effects of new TSPO ligands in a cellular model of tauopathies.Journal of neuroendocrinology · 2020Article
- Microglial Pro-Inflammatory and Anti-Inflammatory Phenotypes Are Modulated by Translocator Protein Activation.International journal of molecular sciences · 2019Article
- Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists.ACS omega · 2018Article
- Central intracrine DHEA synthesis in ageing-related neuroinflammation and neurodegeneration: therapeutic potential?Journal of neuroinflammation · 2018Review
- Leydig cells: formation, function, and regulation.Biology of reproduction · 2018Review
- An Updated View of Translocator Protein (TSPO).International journal of molecular sciences · 2017Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The steroidogenic 18 kDa translocator protein (TSPO) is an emerging, attractive therapeutic tool for several pathological conditions of the nervous system. Here, 13 high affinity TSPO ligands belonging to our previously described N,N-dialkyl-2-phenylindol-3-ylglyoxylamide (PIGA) class were evaluated for their potential ability to affect the cellular Oxidative Metabolism Activity/Proliferation index, which is used as a measure of astrocyte well-being. The most active PIGA ligands were also assessed for steroidogenic activity in terms of pregnenolone production, and the values were related to the metabolic index in rat and human models. The results showed a positive correlation between the increase in the Oxidative Metabolism Activity/Proliferation index and the pharmacologically induced stimulation of steroidogenesis. The specific involvement of steroid molecules in mediating the metabolic effects of the PIGA ligands was demonstrated using aminoglutethimide, a specific inhibitor of the first step of steroid biosynthesis. The most promising steroidogenic PIGA ligands were the 2-naphthyl derivatives that showed a long residence time to the target, in agreement with our previous data. In conclusion, TSPO ligand-induced neurosteroidogenesis was involved in astrocyte well-being.
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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.