ArticleACS chemical neuroscience2015
Characterization of novel cannabinoid based T-type calcium channel blockers with analgesic effects.
Article in ACS chemical neuroscience, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 46 citations in OpenAlex.
- The Increased Activity of CaV3.2 Channels Contributes to Nociceptors' Hyperexcitability and Chronic Neuropathic Pain Following Spinal Cord Injury in Mice.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2026Article
- Cannabinoids activate the insulin pathway to modulate mobilization of cholesterol in C. elegans.PLoS genetics · 2022Article
- The intersection of astrocytes and the endocannabinoid system in the lateral habenula: on the fast-track to novel rapid-acting antidepressants.Molecular psychiatry · 2022Review
- Central and peripheral contributions of T-type calcium channels in pain.Molecular brain · 2022Review
- Theoretical Study of the Structural Stability, Chemical Reactivity, and Protein Interaction for NMP Compounds as Modulators of the Endocannabinoid System.Molecules (Basel, Switzerland) · 2022Article
- Conceptual DFT, QTAIM, and Molecular Docking Approaches to Characterize the T-Type Calcium Channel Blocker Anandamide.Frontiers in chemistry · 2022Article
- Synthesis of Cannabinoids: "In Water" and "On Water" Approaches: Influence of SDS Micelles.The Journal of organic chemistry · 2021Article
- Peripheral Voltage-Gated Cation Channels in Neuropathic Pain and Their Potential as Therapeutic Targets.Frontiers in pain research (Lausanne, Switzerland) · 2021Review
- Change in Cav3.2 T-Type Calcium Channel Induced by Varicella-Zoster Virus Participates in the Maintenance of Herpetic Neuralgia.Frontiers in neurology · 2021Article
- Cav3.2 T-type calcium channels control acute itch in mice.Molecular brain · 2020Article
- Recent advances in the development of T-type calcium channel blockers for pain intervention.British journal of pharmacology · 2018Review
- Inhibition of human N- and T-type calcium channels by an ortho-phenoxyanilide derivative, MONIRO-1.British journal of pharmacology · 2018Article
- Sub-synaptic localization of CaBrain structure & function · 2017Article
- Discovery and mode of action of a novel analgesic β-toxin from the African spider Ceratogyrus darlingi.PloS one · 2017Article
- Effect of the T-type channel blocker KYS-05090S in mouse models of acute and neuropathic pain.Pflugers Archiv : European journal of physiology · 2016Article
- Synthesis and characterization of a disubstituted piperazine derivative with T-type channel blocking action and analgesic properties.Molecular pain · 2016Article
- Targeting voltage-gated calcium channels in neurological and psychiatric diseases.Nature reviews. Drug discovery · 2016Review
- Zinc regulates a key transcriptional pathway for epileptogenesis via metal-regulatory transcription factor 1.Nature communications · 2015Article
- The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential.Pharmacological reviews · 2015Review
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Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
Low-voltage-activated (T-type) calcium channels are important regulators of the transmission of nociceptive information in the primary afferent pathway and finding ligands that modulate these channels is a key focus of the drug discovery field. Recently, we characterized a set of novel compounds with mixed cannabinoid receptor/T-type channel blocking activity and examined their analgesic effects in animal models of pain. Here, we have built on these previous findings and synthesized a new series of small organic compounds. We then screened them using whole-cell voltage clamp techniques to identify the most potent T-type calcium channel inhibitors. The two most potent blockers (compounds 9 and 10) were then characterized using radioligand binding assays to determine their affinity for CB1 and CB2 receptors. The structure-activity relationship and optimization studies have led to the discovery of a new T-type calcium channel blocker, compound 9. Compound 9 was efficacious in mediating analgesia in mouse models of acute inflammatory pain and in reducing tactile allodynia in the partial nerve ligation model. This compound was shown to be ineffective in Cav3.2 T-type calcium channel null mice at therapeutically relevant concentrations, and it caused no significant motor deficits in open field tests. Taken together, our data reveal a novel class of compounds whose physiological and therapeutic actions are mediated through block of Cav3.2 calcium channels.
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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.