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  • Article
  • Open Access
3 Citations
3,906 Views
16 Pages

4-Oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione Derivatives as NMDA Receptor- and VGCC Blockers with Neuroprotective Potential

  • Ayodeji O. Egunlusi,
  • Sarel F. Malan,
  • Sylvester I. Omoruyi,
  • Okobi E. Ekpo and
  • Jacques Joubert

5 October 2020

The impact of excitotoxicity mediated by N-methyl-D-aspartate (NMDA) receptor overactivation and voltage gated calcium channel (VGCC) depolarization is prominent among the postulated processes involved in the development of neurodegenerative disorder...

  • Review
  • Open Access
889 Views
27 Pages

Centrally Acting Skeletal Muscle Relaxants Sharing Molecular Targets with Drugs for Neuropathic Pain Management

  • Judit Mária Kirchlechner-Farkas,
  • David Arpad Karadi,
  • Imre Boldizsár,
  • Nariman Essmat,
  • Anna Rita Galambos,
  • Zoltán Patrik Lincmajer,
  • Sarah Kadhim Abbood,
  • Kornél Király,
  • Éva Szökő and
  • Mahmoud Al-Khrasani
  • + 1 author

31 December 2025

Treatment of neuropathic pain (NP) remains a challenge in clinical practice because the current treatment approaches produce satisfactory pain alleviation in only 30% of patients. This necessitates developing novel drugs or repurposing existing medic...

  • Article
  • Open Access
3 Citations
2,982 Views
13 Pages

30 March 2021

The suitability of a newly developed cell-based functional assay was tested for the detection of the activity of a range of neurotoxins and neuroactive pharmaceuticals which act by stimulation or inhibition of calcium-dependent neurotransmitter relea...

  • Article
  • Open Access
33 Citations
9,453 Views
15 Pages

Fluoxetine Suppresses Glutamate- and GABA-Mediated Neurotransmission by Altering SNARE Complex

  • Vesna Lazarevic,
  • Ioannis Mantas,
  • Ivana Flais and
  • Per Svenningsson

30 August 2019

Major depressive disorder is one of the most common neuropsychiatric disorders worldwide. The treatment of choice that shows good efficacy in mood stabilization is based on selective serotonin reuptake inhibitors (SSRIs). Their primary mechanism of a...

  • Review
  • Open Access
16 Citations
8,465 Views
37 Pages

Marine Toxins and Nociception: Potential Therapeutic Use in the Treatment of Visceral Pain Associated with Gastrointestinal Disorders

  • Andreina Baj,
  • Michela Bistoletti,
  • Annalisa Bosi,
  • Elisabetta Moro,
  • Cristina Giaroni and
  • Francesca Crema

31 July 2019

Visceral pain, of which the pathogenic basis is currently largely unknown, is a hallmark symptom of both functional disorders, such as irritable bowel syndrome, and inflammatory bowel disease. Intrinsic sensory neurons in the enteric nervous system a...

  • Opinion
  • Open Access
3 Citations
2,474 Views
8 Pages

The Clinical Concept of LTDpathy: Is Dysregulated LTD Responsible for Prodromal Cerebellar Symptoms?

  • Hiroshi Mitoma,
  • Kazuhiko Yamaguchi,
  • Jerome Honnorat and
  • Mario Manto

24 February 2022

Long-term depression at parallel fibers-Purkinje cells (PF-PC LTD) is essential for cerebellar motor learning and motor control. Recent progress in ataxiology has identified dysregulation of PF-PC LTD in the pathophysiology of certain types of immune...

  • Review
  • Open Access
12 Citations
4,610 Views
24 Pages

30 November 2022

Voltage-gated calcium channels (VGCCs) and estrogen receptors are important cellular proteins that have been shown to interact with each other across varied cells and tissues. Estrogen hormone, the ligand for estrogen receptors, can also exert its ef...

  • Article
  • Open Access
2 Citations
2,694 Views
18 Pages

Conditional Knockout of Neurexins Alters the Contribution of Calcium Channel Subtypes to Presynaptic Ca2+ Influx

  • Johannes Brockhaus,
  • Iris Kahl,
  • Mohiuddin Ahmad,
  • Daniele Repetto,
  • Carsten Reissner and
  • Markus Missler

5 June 2024

Presynaptic Ca2+ influx through voltage-gated Ca2+ channels (VGCCs) is a key signal for synaptic vesicle release. Synaptic neurexins can partially determine the strength of transmission by regulating VGCCs. However, it is unknown whether neurexins mo...

  • Review
  • Open Access
18 Citations
9,038 Views
17 Pages

Current Drug Development Overview: Targeting Voltage-Gated Calcium Channels for the Treatment of Pain

  • Flavia Tasmin Techera Antunes,
  • Maria Martha Campos,
  • Vanice de Paula Ricardo Carvalho,
  • Claudio Antonio da Silva Junior,
  • Luiz Alexandre Viana Magno,
  • Alessandra Hubner de Souza and
  • Marcus Vinicius Gomez

Voltage-gated calcium channels (VGCCs) are targeted to treat pain conditions. Since the discovery of their relation to pain processing control, they are investigated to find new strategies for better pain control. This review provides an overview of...

  • Review
  • Open Access
22 Citations
11,041 Views
20 Pages

15 February 2022

Voltage-gated calcium channels (VGCCs) are widely expressed in the brain, heart and vessels, smooth and skeletal muscle, as well as in endocrine cells. VGCCs mediate gene transcription, synaptic and neuronal structural plasticity, muscle contraction,...

  • Feature Paper
  • Review
  • Open Access
88 Citations
8,010 Views
17 Pages

21 September 2020

Aggregation and deposition of β-amyloid and/or tau protein are the key neuropathological features in neurodegenerative disorders such as Alzheimer’s disease (AD) and other tauopathies including frontotemporal dementia (FTD). The interactio...

  • Review
  • Open Access
9 Citations
3,708 Views
13 Pages

Many exogenous and endogenous risk factors have been proposed as precursors of brain tumors, including the exposure to non-ionizing electromagnetic fields. Nevertheless, there is still a debate among the scientific community about the hazard of the e...

  • Review
  • Open Access
17 Citations
6,396 Views
17 Pages

20 February 2020

Background: Neurodegenerative and mood disorders represent growing medical and social problems, many of which are provoked by oxidative stress, disruption in the metabolism of various neurotransmitters, and disturbances in calcium homeostasis. Biolog...

  • Review
  • Open Access
24 Citations
8,685 Views
59 Pages

Intracellular Ca2+ distribution is a tightly regulated process. Numerous Ca2+ chelating, storage, and transport mechanisms are required to maintain normal cellular physiology. Ca2+-binding proteins, mainly calmodulin and calbindins, sequester free in...

  • Article
  • Open Access
14 Citations
3,576 Views
16 Pages

The Effect of Isosaponarin Derived from Wasabi Leaves on Glutamate Release in Rat Synaptosomes and Its Underlying Mechanism

  • Cheng-Wei Lu,
  • Kun-Chieh Yeh,
  • Kuan-Ming Chiu,
  • Ming-Yi Lee,
  • Tzu-Yu Lin and
  • Su-Jane Wang

Excessive glutamate release is known to be involved in the pathogenesis of neurological diseases, and suppression of glutamate release from nerve terminals is considered to be a treatment strategy. In this study, we investigated whether isosaponarin,...

  • Article
  • Open Access
3 Citations
4,469 Views
23 Pages

31 August 2022

N-methyl-D-aspartate (NMDA) receptors play a critical role in activity-dependent dendritic arborization, spinogenesis, and synapse formation by stimulating calcium-dependent signaling pathways. Previously, we have shown that brevetoxin 2 (PbTx-2), a...

  • Article
  • Open Access
3 Citations
2,126 Views
17 Pages

Far-Infrared Ameliorates Pb-Induced Renal Toxicity via Voltage-Gated Calcium Channel-Mediated Calcium Influx

  • Chin-Meng Ko,
  • Chee-Kin Then,
  • Yu-Ming Kuo,
  • Yen-Kuang Lin and
  • Shing-Chuan Shen

31 October 2023

Far-infrared (FIR), characterized by its specific electromagnetic wavelengths, has emerged as an adjunctive therapeutic strategy for various diseases, particularly in ameliorating manifestations associated with renal disorders. Although FIR was confi...

  • Article
  • Open Access
12 Citations
3,893 Views
16 Pages

18 October 2021

Reduction in glutamate release is a key mechanism for neuroprotection and we investigated the effect of isoliquiritigenin (ISL), an active ingredient of Glycyrrhiza with neuroprotective activities, on glutamate release in rat cerebrocortical nerve te...

  • Article
  • Open Access
23 Citations
4,688 Views
14 Pages

Role of L-Type Voltage-Gated Calcium Channels in Epileptiform Activity of Neurons

  • Denis P. Laryushkin,
  • Sergei A. Maiorov,
  • Valery P. Zinchenko,
  • Sergei G. Gaidin and
  • Artem M. Kosenkov

25 September 2021

Epileptic discharges manifest in individual neurons as abnormal membrane potential fluctuations called paroxysmal depolarization shift (PDS). PDSs can combine into clusters that are accompanied by synchronous oscillations of the intracellular Ca2+ co...

  • Article
  • Open Access
8 Citations
4,117 Views
12 Pages

26 February 2020

TMEM16A/anoctamin1 (ANO1), a calcium (Ca2+)-activated chloride (Cl) channel, has many functions in various excitable cells and modulates excitability in both Ca2+- and voltage-gating modes. However, its gating characteristics and role in prima...

  • Article
  • Open Access
9 Citations
2,691 Views
19 Pages

27 October 2022

The α2δ subunit is a high-voltage activated (HVA) calcium channel (Cav1 and Cav2) auxiliary subunit that increases the density and function of HVA calcium channels in the plasma membrane of mammals. However, its function in plant parasiti...

  • Review
  • Open Access
74 Citations
22,849 Views
25 Pages

Voltage-Gated Calcium Channel Antagonists and Traumatic Brain Injury

  • Gene Gurkoff,
  • Kiarash Shahlaie,
  • Bruce Lyeth and
  • Robert Berman

26 June 2013

Traumatic brain injury (TBI) is a leading cause of death and disability in the United States. Despite more than 30 years of research, no pharmacological agents have been identified that improve neurological function following TBI. However, several li...

  • Review
  • Open Access
15 Citations
8,582 Views
18 Pages

27 May 2013

Membrane-bound voltage-gated Ca2+ channels (VGCCs) are targets for specific signaling complexes, which regulate important processes like gene expression, neurotransmitter release and neuronal excitability. It is becoming increasingly evident that the...

  • Article
  • Open Access
769 Views
18 Pages

21 October 2025

Melicoccus bijugatus (Guinep) is traditionally consumed in the Caribbean and Latin America for its health benefits, yet its cardiovascular effects remain underexplored. This study investigated the therapeutic potential of Guinep by combining experime...

  • Article
  • Open Access
6 Citations
2,784 Views
15 Pages

10 December 2020

How ion channels impact the response of the ocular surface to dry eye is only beginning to be explored. Here, we review recent progress and provide new experimental data clarifying the exocytosis-altering actions of ion channels in conjunctival goble...

  • Feature Paper
  • Article
  • Open Access
1,477 Views
21 Pages

Identification of CaVβ1 Isoforms Required for Neuromuscular Junction Formation and Maintenance

  • Amélie Vergnol,
  • Aly Bourguiba,
  • Stephanie Bauché,
  • Massiré Traoré,
  • Maxime Gelin,
  • Christel Gentil,
  • Sonia Pezet,
  • Lucile Saillard,
  • Pierre Meunier and
  • Sestina Falcone
  • + 8 authors

6 August 2025

Voltage-gated Ca2+ channels (VGCCs) are regulated by four CaVβ subunits (CaVβ1–CaVβ4), each showing specific expression patterns in excitable cells. While primarily known for regulating VGCC function, CaVβ proteins also have...

  • Article
  • Open Access
21 Citations
4,515 Views
17 Pages

Repositioning Trimebutine Maleate as a Cancer Treatment Targeting Ovarian Cancer Stem Cells

  • Heejin Lee,
  • Oh-Bin Kwon,
  • Jae-Eon Lee,
  • Yong-Hyun Jeon,
  • Dong-Seok Lee,
  • Sang-Hyun Min and
  • Jun-Woo Kim

16 April 2021

The overall five-year survival rate for late-stage patients of ovarian cancer is below 29% due to disease recurrence and drug resistance. Cancer stem cells (CSCs) are known as a major contributor to drug resistance and recurrence. Accordingly, therap...

  • Article
  • Open Access
12 Citations
4,067 Views
21 Pages

Inherited Retinal Degeneration: PARP-Dependent Activation of Calpain Requires CNG Channel Activity

  • Jie Yan,
  • Alexander Günter,
  • Soumyaparna Das,
  • Regine Mühlfriedel,
  • Stylianos Michalakis,
  • Kangwei Jiao,
  • Mathias W. Seeliger and
  • François Paquet-Durand

15 March 2022

Inherited retinal degenerations (IRDs) are a group of blinding diseases, typically involving a progressive loss of photoreceptors. The IRD pathology is often based on an accumulation of cGMP in photoreceptors and associated with the excessive activat...

  • Editorial
  • Open Access
6 Citations
3,137 Views
8 Pages

19 September 2023

Signals of nerve impulses are transmitted to excitatory cells to induce the action of organs via the activation of Ca2+ entry through voltage-gated Ca2+ channels (VGCC), which are classified based on their activation threshold into high- and low-volt...

  • Review
  • Open Access
29 Citations
11,416 Views
12 Pages

Mirogabalin—A Novel Selective Ligand for the α2δ Calcium Channel Subunit

  • Renata Zajączkowska,
  • Joanna Mika,
  • Wojciech Leppert,
  • Magdalena Kocot-Kępska,
  • Małgorzata Malec-Milewska and
  • Jerzy Wordliczek

31 January 2021

The efficacy of neuropathic pain control remains unsatisfactory. Despite the availability of a variety of therapies, a significant proportion of patients suffer from poorly controlled pain of this kind. Consequently, new drugs and treatments are stil...

  • Article
  • Open Access
6 Citations
3,042 Views
16 Pages

The voltage-gated calcium channel (VGCC) β subunit (Cavβ) protein is a kind of cytosolic auxiliary subunit that plays an important role in regulating the surface expression and gating characteristics of high-voltage-activated (HVA) calcium...

  • Article
  • Open Access
3 Citations
3,050 Views
15 Pages

Vascular Response of Tetrabromobisphenol a in Rat Aorta: Calcium Channels Inhibition and Potassium Channels Activation

  • Joana Feiteiro,
  • Sandra M. Rocha,
  • Melissa Mariana,
  • Cláudio J. Maia and
  • Elisa Cairrao

9 September 2022

Tetrabromobisphenol A (TBBPA) is a flame retardant widely used to reduce flammability. It is an endocrine disruptor, and due to constant human exposure, some concerns have been raised regarding its impact on human health. Studies showed that TBBPA af...

  • Article
  • Open Access
3 Citations
2,584 Views
24 Pages

28 October 2022

Unidentified pathogenetic mechanisms and genetic and clinical heterogeneity represent critical factors hindering the development of treatments for inherited retinal dystrophies. Frameshift mutations in Cacna2d4, which codes for an accessory subunit o...

  • Article
  • Open Access
11 Citations
4,151 Views
31 Pages

11 July 2022

Neurotransmitter release from presynaptic terminals is primarily regulated by rapid Ca2+ influx through membrane-resident voltage-gated Ca2+ channels (VGCCs). Moreover, accumulating evidence indicates that the endoplasmic reticulum (ER) is extensivel...

  • Article
  • Open Access
9 Citations
4,291 Views
13 Pages

Altered Calcium Influx Pathways in Cancer-Associated Fibroblasts

  • Francisco Sadras,
  • Teneale A. Stewart,
  • Mélanie Robitaille,
  • Amelia A. Peters,
  • Priyakshi Kalita-de Croft,
  • Patsy S. Soon,
  • Jodi M. Saunus,
  • Sunil R. Lakhani,
  • Sarah J. Roberts-Thomson and
  • Gregory R. Monteith

Cancer-associated fibroblasts (CAFs) represent an important component of the tumour microenvironment and are implicated in disease progression. Two outstanding questions in cancer biology are how CAFs arise and how they might be targeted therapeutica...

  • Review
  • Open Access
20 Citations
6,460 Views
31 Pages

In the last years, different kinds of limbic encephalitis associated with autoantibodies against ion channels and synaptic receptors have been described. Many studies have demonstrated that such autoantibodies induce channel or receptor dysfunction....

  • Communication
  • Open Access
5 Citations
2,686 Views
10 Pages

1 September 2023

Acute hyperglycemia induces oxidative damage and inflammation, leading to vascular dysfunction. Ginsenoside Rb1 (Rb1) is a major component of red ginseng with anti-diabetic, anti-oxidant and anti-inflammatory properties. Here, we investigated the ben...

  • Article
  • Open Access
13 Citations
3,350 Views
15 Pages

Electrical Stimulation Therapy and HA/TCP Composite Scaffolds Modulate the Wnt Pathways in Bone Regeneration of Critical-Sized Defects

  • Júlia Venturini Helaehil,
  • Luiza Venturini Helaehil,
  • Laryssa Fernanda Alves,
  • Boyang Huang,
  • Milton Santamaria-Jr,
  • Paulo Bartolo and
  • Guilherme Ferreira Caetano

Critical bone defects are the most difficult challenges in the area of tissue repair. Polycaprolactone (PCL) scaffolds, associated with hydroxyapatite (HA) and tricalcium phosphate (TCP), are reported to have an enhanced bioactivity. Moreover, the us...

  • Communication
  • Open Access
5 Citations
2,221 Views
14 Pages

Despite combination antiretroviral therapy, HIV-associated neurocognitive disorders (HAND) occur in ~50% of people living with HIV (PLWH), which are associated with dysfunction of the corticostriatal pathway. The mechanism by which HIV alters the neu...

  • Review
  • Open Access
41 Citations
9,074 Views
8 Pages

15 November 2017

Voltage-gated calcium channels (VGCCs) are widely distributed within the central nervous system (CNS) and presumed to play an important role in the pathophysiology of a broad spectrum of CNS disorders including Alzheimer’s and Parkinson’s disease as...

  • Communication
  • Open Access
3 Citations
2,421 Views
11 Pages

Mammalian Brain Ca2+ Channel Activity Transplanted into Xenopus laevis Oocytes

  • Matthieu Rousset,
  • Sandrine Humez,
  • Cyril Laurent,
  • Luc Buée,
  • David Blum,
  • Thierry Cens,
  • Michel Vignes and
  • Pierre Charnet

Several mutations on neuronal voltage-gated Ca2+ channels (VGCC) have been shown to cause neurological disorders and contribute to the initiation of epileptic seizures, migraines, or cerebellar degeneration. Analysis of the functional consequences of...

  • Article
  • Open Access
29 Citations
9,870 Views
13 Pages

Modulation of Ca2+ Signals by Epigallocatechin-3-gallate(EGCG) in Cultured Rat Hippocampal Neurons

  • Jiang-Hua Wang,
  • Jin Cheng,
  • Cai-Rong Li,
  • Mao Ye,
  • Zhe Ma and
  • Fei Cai

20 January 2011

Green tea has been receiving considerable attention as a possible neuroprotective agent against neurodegenerative disease. Epigallocatechin-3-gallate (EGCG) is the major compound of green tea. Calcium signaling has profound effects on almost all aspe...

  • Article
  • Open Access
15 Citations
4,540 Views
16 Pages

Investigation of Ultrasound-Mediated Intracellular Ca2+ Oscillations in HIT-T15 Pancreatic β-Cell Line

  • Chi Woo Yoon,
  • Nan Sook Lee,
  • Kweon Mo Koo,
  • Sunho Moon,
  • Kyosuk Goo,
  • Hayong Jung,
  • Changhan Yoon,
  • Hae Gyun Lim and
  • K. Kirk Shung

4 May 2020

In glucose-stimulated insulin secretion (GSIS) of pancreatic β-cells, the rise of free cytosolic Ca2+ concentration through voltage-gated calcium channels (VGCCs) triggers the exocytosis of insulin-containing granules. Recently, mechanically ind...

  • Article
  • Open Access
24 Citations
5,701 Views
15 Pages

Suramin-Induced Neurotoxicity: Preclinical Models and Neuroprotective Strategies

  • David Von der Ahe,
  • Petra Huehnchen,
  • Mustafa Balkaya,
  • Sarah Peruzzaro,
  • Matthias Endres and
  • Wolfgang Boehmerle

7 February 2018

Suramin is a trypan blue analogon originally developed to treat protozoan infections, which was found to have diverse antitumor effects. One of the most severe side effects in clinical trials was the development of a peripheral sensory-motor polyneur...

  • Review
  • Open Access
18 Citations
7,103 Views
35 Pages

The Alteration of Microglial Calcium Homeostasis in Central Nervous System Disorders: A Comprehensive Review

  • Al Riyad Hasan,
  • Faria Tasnim,
  • Md. Aktaruzzaman,
  • Md. Tarikul Islam,
  • Rifat Rayhan,
  • Afrina Brishti,
  • Junguk Hur,
  • James E. Porter and
  • Md. Obayed Raihan

21 October 2024

Microglia, the unique and motile immune cells of the central nervous system (CNS), function as a security guard in maintaining CNS homeostasis, primarily through calcium signaling. The calcium dynamics in microglia control important functions such as...

  • Review
  • Open Access
1 Citations
9,641 Views
38 Pages

The roles of perinatal development, intracellular calcium [Ca2+]i, and synaptogenesis disruption are not novel in the autism/ASD literature. The focus on six mechanisms controlling synaptogenesis, each regulated by [Ca2+]i, and each aberrant in ASDs...

  • Review
  • Open Access
20 Citations
5,773 Views
20 Pages

27 March 2024

Originally developed as a chemotherapeutic agent, miltefosine (hexadecylphosphocholine) is an inhibitor of phosphatidylcholine synthesis with proven antiparasitic effects. It is the only oral drug approved for the treatment of Leishmaniasis and Ameri...

  • Review
  • Open Access
26 Citations
15,304 Views
19 Pages

Investigational Drugs for the Treatment of Postherpetic Neuralgia: Systematic Review of Randomized Controlled Trials

  • Miguel Á. Huerta,
  • Miguel M. Garcia,
  • Beliu García-Parra,
  • Ancor Serrano-Afonso and
  • Nancy Paniagua

20 August 2023

The pharmacological treatment of postherpetic neuralgia (PHN) is unsatisfactory, and there is a clinical need for new approaches. Several drugs under advanced clinical development are addressed in this review. A systematic literature search was condu...

  • Review
  • Open Access
16 Citations
6,887 Views
28 Pages

The Puzzling Role of Neuron-Specific PMCA Isoforms in the Aging Process

  • Tomasz Boczek,
  • Tomasz Radzik,
  • Bozena Ferenc and
  • Ludmila Zylinska

16 December 2019

The aging process is a physiological phenomenon associated with progressive changes in metabolism, genes expression, and cellular resistance to stress. In neurons, one of the hallmarks of senescence is a disturbance of calcium homeostasis that may ha...

  • Review
  • Open Access
66 Citations
8,514 Views
24 Pages

Sperm motility is linked to the activation of signaling pathways that trigger movement. These pathways are mainly dependent on Ca2+, which acts as a secondary messenger. The maintenance of adequate Ca2+ concentrations is possible thanks to proper con...

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