ArticleScientific reports2016
Sigma-1 Receptor Agonism Promotes Mechanical Allodynia After Priming the Nociceptive System with Capsaicin.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 32 citations in OpenAlex.
- The SigmaPharmacological reports : PR · 2026Article
- The LRP1-SHP2 pathway regulates TRPV1 sensitivity in the peripheral nervous system: Insights from amyloid beta 1-42 modulation.Journal of advanced research · 2026Article
- 2-{International journal of molecular sciences · 2025Article
- Efficacy of the Multi-Target Compound E153 in Relieving Pain and Pruritus of Different Origins.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Discovery of RC-752, a Novel Sigma-1 Receptor Antagonist with Antinociceptive Activity: A Promising Tool for Fighting Neuropathic Pain.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Article
- Impact of Two Neuronal Sigma-1 Receptor Modulators, PRE084 and DMT, on Neurogenesis and Neuroinflammation in an AβInternational journal of molecular sciences · 2022Article
- Sigma-1 receptor activity in primary sensory neurons is a critical driver of neuropathic pain.Gene therapy · 2022Article
- Studies on the affinity of 6-[(RSC medicinal chemistry · 2021Article
- Propellanes as Rigid Scaffolds for the Stereodefined Attachment of σ-Pharmacophoric Structural Elements to Achieve σ Affinity.International journal of molecular sciences · 2021Article
- Progesterone and Allopregnanolone Rapidly Attenuate Estrogen-Associated Mechanical Allodynia in Rats with Persistent Temporomandibular Joint Inflammation.Frontiers in integrative neuroscience · 2020Article
- Novel missense alleles of SIGMAR1 as tools to understand emerin-dependent gene silencing in response to cocaine.Experimental biology and medicine (Maywood, N.J.) · 2019Article
- Sigma-1 Receptor Activation Induces Autophagy and Increases Proteostasis Capacity In Vitro and In Vivo.Cells · 2019Article
- A New Pharmacophore Model for the Design of Sigma-1 Ligands Validated on a Large Experimental Dataset.Frontiers in pharmacology · 2019Article
- Sigma-1 Receptor Inhibition Reduces Neuropathic Pain Induced by Partial Sciatic Nerve Transection in Mice by Opioid-Dependent and -Independent Mechanisms.Frontiers in pharmacology · 2019Article
- Molecular Interplay Between the Sigma-1 Receptor, Steroids, and Ion Channels.Frontiers in pharmacology · 2019Review
- TRPV1 channels and the progesterone receptor Sig-1R interact to regulate pain.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Sigma-1 receptor antagonists promote antinociception in several models of pain, but the effects of sigma-1 agonists on nociception (particularly when the nociceptive system is primed) are not so well characterized; therefore we evaluated the effects of sigma-1 agonists on pain under different experimental conditions. The systemic administration of the selective sigma-1 agonists (+)-pentazocine and PRE-084, as well as the nonselective sigma-1 agonist carbetapentane (used clinically as an antitussive drug), did not alter sensitivity to mechanical stimulation under baseline conditions. However, they greatly promoted secondary mechanical allodynia after priming the nociceptive system with capsaicin. These effects of sigma-1 agonists were consistent in terms potency with the affinities of these drugs for sigma-1 receptors, were reversed by sigma-1 antagonists, and were not observed in sigma-1 knockout mice, indicating that they are sigma-1-mediated. Repeated systemic treatment with PRE-084 induced proallodynic effects even 24 h after treatment completion, but only after the nociceptive system was primed. However, neither the presence of this drug in the organism nor changes in sigma-1 receptor expression in areas involved in pain processing explains its long-term effects, suggesting that sustained sigma-1 agonism induces plastic changes in the nociceptive system that promote nociception.
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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.