ArticlePflugers Archiv : European journal of physiology2015
Analgesic effect of a broad-spectrum dihydropyridine inhibitor of voltage-gated calcium channels.
Article in Pflugers Archiv : European journal of physiology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 39 citations in OpenAlex.
- Depolarization induces nociceptor sensitization by CaV1.2-mediated PKA-II activation.The Journal of cell biology · 2021Article
- Use of Pluronic Surfactants in Gel Formulations of Photosensitive 1,4-Dihydropyridine Derivatives: A Potential Approach in the Treatment of Neuropathic Pain.Pharmaceutics · 2021Article
- Peripheral Voltage-Gated Cation Channels in Neuropathic Pain and Their Potential as Therapeutic Targets.Frontiers in pain research (Lausanne, Switzerland) · 2021Review
- Synthesis of Biologically Active Molecules through Multicomponent Reactions.Molecules (Basel, Switzerland) · 2020Review
- 5-Oxo-hexahydroquinoline: an attractive scaffold with diverse biological activities.Molecular diversity · 2019Review
- A New Generation of Dihydropyridine Calcium Channel Blockers: Photostabilization of Liquid Formulations Using Nonionic Surfactants.Pharmaceutics · 2019Article
- Recent advances in the development of T-type calcium channel blockers for pain intervention.British journal of pharmacology · 2018Review
- Calcium signalling through L-type calcium channels: role in pathophysiology of spinal nociceptive transmission.British journal of pharmacology · 2018Review
- Danger: High Voltage-The Role of Voltage-Gated Calcium Channels in Central Nervous System Pathology.Cells · 2017Review
- Effect of the T-type channel blocker KYS-05090S in mouse models of acute and neuropathic pain.Pflugers Archiv : European journal of physiology · 2016Article
- A cell-permeant peptide corresponding to the cUBP domain of USP5 reverses inflammatory and neuropathic pain.Molecular pain · 2016Article
- Synthesis and characterization of a disubstituted piperazine derivative with T-type channel blocking action and analgesic properties.Molecular pain · 2016Article
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Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
Abstract
Voltage-activated calcium channels are important facilitators of nociceptive transmission in the primary afferent pathway. Consequently, molecules that block these channels are of potential use as pain therapeutics. Our group has recently reported on the identification of a novel class of dihydropyridines (DHPs) that included compounds with preferential selectivity for T-type over L-type channels. Among those compounds, M4 was found to be an equipotent inhibitor of both Cav1.2 L- and Cav3.2 T-type calcium channels. Here, we have further characterized the effects of this compound on other types of calcium channels and examined its analgesic effect when delivered either spinally (i.t.) or systemically (i.p.) to mice. Both delivery routes resulted in antinociception in a model of acute pain. Furthermore, M4 was able to reverse mechanical hyperalgesia produced by nerve injury when delivered intrathecally. M4 retained partial activity when delivered to Cav3.2 null mice, indicating that this compound acts on multiple targets. Additional whole-cell patch clamp experiments in transfected tsA-201 cells revealed that M4 also effectively blocks Cav3.3 (T-type) and Cav2.2 (N-type) currents. Altogether, our data indicate that broad-spectrum inhibition of multiple calcium channel subtypes can lead to potent analgesia in rodents.
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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.