ArticleMolecular pharmacology2011
Verapamil block of T-type calcium channels.
Article in Molecular pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
41 citing papers in PubMed, 83 citations in OpenAlex.
- L-type calcium channel modulation reveals the relationship between neuronal synchrony and hyperactivity in the inferior colliculus following noise-induced hearing loss.Scientific reports · 2025Article
- Substrate recognition diversity and transport dynamics of ABCC1.Nature communications · 2025Article
- The Synaptic and Intrinsic Cellular Mechanisms of Persistent Firing in Neurogliaform Cells.Biomolecules · 2025Article
- The Soil-Plant Continuity of Rare Earth Elements: Insights into an Enigmatic Class of Xenobiotics and Their Interactions with Plant Structures and Processes.Journal of xenobiotics · 2025Review
- Voltage-Gated Calcium Channels and the Parity-Dependent Differential Uterine Response to Oxytocin in Rats.Reproductive sciences (Thousand Oaks, Calif.) · 2025Article
- Flunarizine as a Candidate for Drug Repurposing Against Human Pathogenic Mammarenaviruses.Viruses · 2025Article
- Pre-cluster symptoms in a Taiwanese cohort of cluster headache: symptom profiles and clinical predictions.The journal of headache and pain · 2024Article
- T- and L-Type Calcium Channels Maintain Calcium Oscillations in the Murine Zona Glomerulosa.Hypertension (Dallas, Tex. : 1979) · 2024Article
- Diminished NAD+ levels and activation of retrotransposons promote postovulatory aged oocyte (POAO) death.Cell death discovery · 2024Article
- Cytoplasmic CaFrontiers in plant science · 2024Article
- Verapamil inhibits Kir2.3 channels by binding to the pore and interfering with PIPNaunyn-Schmiedeberg's archives of pharmacology · 2023Article
- T-type calcium channels as therapeutic targets in essential tremor and Parkinson's disease.Annals of clinical and translational neurology · 2023Review
- Rescue of lysosomal function as therapeutic strategy for SPG15 hereditary spastic paraplegia.Brain : a journal of neurology · 2023Article
- Ion channels as molecular targets of glioblastoma electrotherapy.Frontiers in cellular neuroscience · 2023Review
- Verapamil chronicles: advances from cardiovascular to pancreatic β-cell protection.Frontiers in pharmacology · 2023Review
- T-Type Calcium Channels: A Mixed Blessing.International journal of molecular sciences · 2022Review
- The CaPharmaceutics · 2022Article
- Investigation of the effect of verapamil on the regional absorption of sofosbuvir from rabbit intestine in situ.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2022Article
- Antiarrhythmic calcium channel blocker verapamil inhibits trek currents in sympathetic neurons.Frontiers in pharmacology · 2022Article
- Role of calcium in hormone-independent and -resistant breast cancer.International journal of cancer · 2021Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Verapamil is a prototypical phenylalkylamine (PAA), and it was the first calcium channel blocker to be used clinically. It tonically blocks L-type channels in the inner pore with micromolar affinity, and its affinity increases at depolarized membrane potentials. In T-type calcium channels, verapamil blocks with micromolar affinity and has modestly increased affinity at depolarized potentials. We found that a related PAA, 4-desmethoxyverapamil (D888), is comparable with verapamil both in affinity and in state-dependence. Permanently charged verapamil was more effective intracellularly than neutral verapamil. Charged PAAs were able to access their binding site from both inside and outside the cell. Furthermore, membrane-impermeant [2-(trimethylammonium)ethyl]methanethiosulfonate was able to access the inner pore from outside of the cell. We examined a homology model of the T-type calcium channel to look for possible routes of drug entry. Mutation of L1825W produced a channel that was blocked significantly more slowly by charged verapamil from the outside, with an increase in apparent affinity when the drug was applied from the inside. Data suggest that T-type channels have a back pathway through which charged drugs can access the inner pore of the channel without passing through the plasma membrane.
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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.