Target intelligence / Profile preview

Voltage-gated and receptor-operated calcium channels (VGCC/ROCC)

Target
VGCC/ROCC
Molecular classification
Ion channel, Voltage-gated ion channel, Ligand-gated ion channel, Receptor
01

Overview

Voltage-gated and receptor-operated calcium channels are essential membrane proteins that facilitate the entry of calcium ions (Ca2+) into cells, acting as key transducers of electrical and chemical signals. Voltage-gated calcium channels (VGCCs) respond to membrane depolarization and are classified into several subtypes (L, T, N, P/Q, and R) that mediate functions such as muscle contraction, neurotransmitter release, and pacemaking (Catterall, 2011). Receptor-operated calcium channels (ROCCs) are activated by the binding of extracellular ligands or through intracellular signaling cascades, playing vital roles in synaptic transmission and cellular homeostasis (Putney, 1990). These channels are critical in the pathophysiology of various conditions, including hypertension, cardiac arrhythmias, chronic pain, and neurodegenerative disorders (StatPearls, 2023). Pharmacological agents targeting VGCCs, such as dihydropyridines, are widely used to manage cardiovascular diseases by inducing vasodilation and reducing cardiac workload. Meanwhile, modulators of ROCCs, such as NMDA receptor antagonists, are employed in treating neurological conditions and as anesthetic agents (IUPHAR/BPS Guide to Pharmacology).

Other names
VOCCROCCVoltage-dependent calcium channelsLigand-gated calcium channelsCalcium channels
02

Mechanism of action

Inhibition of calcium ion influx through the channel pore or modulation of channel gating to decrease intracellular calcium levels and attenuate downstream physiological responses.

03

Biological functions

Signal transductionMuscle contractionNeurotransmissionHormone secretionGene expression
04

Disease associations

Cardiovascular diseaseHypertensionChronic painEpilepsyNeurodegenerative disease
05

Safety considerations

Peripheral edemaHypotensionBradycardiaConstipationDizzinessCNS depression
06

Interacting drugs

Amlodipine

7 more in the full profile.

07

Biomarkers

Blood pressureHeart rateElectrocardiogram (ECG) parametersSeizure frequencyPain intensity scales

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