Target intelligence / Profile preview

L-type voltage-gated calcium channel alpha 1C subunit (Cav1.2)

Target
Cav1.2
Molecular classification
Ion channel, Voltage-gated ion channel, Calcium channel
01

Overview

The L-type voltage-gated calcium channel, specifically the Cav1.2 isoform encoded by the CACNA1C gene, is a critical mediator of electromechanical coupling in gastrointestinal smooth muscle. These channels open in response to membrane depolarization, allowing an influx of extracellular calcium ions that trigger the contractile apparatus of the smooth muscle cells. This process is fundamental to peristalsis and the regulation of gastrointestinal motility. In various motility disorders, such as irritable bowel syndrome (IBS) or achalasia, the activity of these channels may be dysregulated, leading to spasms or impaired transit. Pharmacological targeting of these channels with calcium channel blockers (CCBs) is a common therapeutic strategy to induce smooth muscle relaxation and alleviate pain. While systemic CCBs like nifedipine are used for cardiovascular indications, gut-selective agents like pinaverium are preferred for GI disorders to minimize systemic side effects such as hypotension.

Other names
CACNA1CL-type calcium channelDihydropyridine receptorVoltage-dependent L-type calcium channel subunit alpha-1CCalcium channel, voltage-dependent, L type, alpha 1C subunit
02

Mechanism of action

L-type calcium channel antagonist (blocker) that inhibits the influx of calcium ions into smooth muscle cells, leading to muscle relaxation.

03

Biological functions

Muscle contractionSignal transductionElectromechanical couplingCalcium homeostasisRegulation of membrane potential
04

Disease associations

Irritable bowel syndromeGastrointestinal motility disordersAchalasiaHypertensionArrhythmia
05

Safety considerations

HypotensionPeripheral edemaConstipationBradycardiaGastroesophageal reflux
06

Interacting drugs

Nifedipine

6 more in the full profile.

07

Biomarkers

Intracellular calcium levelsGastrointestinal transit timeManometry pressure readings

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