Target intelligence / Profile preview

Voltage-gated calcium channel (L-type and T-type) (VGCC)

Target
VGCC
Molecular classification
Ion channel, Voltage-gated ion channel
01

Overview

Voltage-gated calcium channels (VGCCs) are essential transmembrane proteins that regulate the influx of calcium ions into cells following membrane depolarization (IUPHAR/BPS Guide to Pharmacology, 2023). This grouping encompasses two distinct functional classes: L-type (Long-lasting) channels, which are high-voltage-activated (HVA), and T-type (Transient) channels, which are low-voltage-activated (LVA) (StatPearls, 2023). L-type channels (Cav1.1–Cav1.4) are predominantly expressed in muscle and endocrine cells, where they trigger muscle contraction and hormone secretion (UniProt, 2023). T-type channels (Cav3.1–Cav3.3) activate at more negative potentials and play a key role in regulating rhythmic electrical activity in the heart and central nervous system (PubMed, PMID: 11160518). Dysfunction in these channels is associated with a variety of conditions, including hypertension, cardiac arrhythmias, and absence seizures (NIH, 2023). Therapeutic agents known as calcium channel blockers (CCBs) target these proteins to manage cardiovascular and neurological disorders by reducing vascular resistance or dampening neuronal hyperexcitability (StatPearls, 2023).

Other names
L-type calcium channelT-type calcium channelLow-voltage-activated calcium channelHigh-voltage-activated calcium channelCav1Cav3VGCC
02

Mechanism of action

Inhibition of calcium ion influx through the channel pore in response to membrane depolarization, thereby reducing intracellular calcium concentrations and modulating cellular excitability and contractility (StatPearls, 2023).

03

Biological functions

Signal transductionMuscle contractionNeurotransmitter releaseCardiac pacemakingGene expression
04

Disease associations

HypertensionAngina pectorisCardiac arrhythmiaEpilepsyChronic painHyperaldosteronism
05

Safety considerations

HypotensionPeripheral edemaBradycardiaAtrioventricular blockGingival hyperplasiaConstipation
06

Interacting drugs

Amlodipine

7 more in the full profile.

07

Biomarkers

Blood pressureHeart rateElectrocardiogram (ECG) PR intervalIntracellular calcium transients

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