Target intelligence / Profile preview

Voltage-gated calcium channel subunit alpha-1 (L-type) (CaV1.x (where x specifies the subtype, e.g., CaV1.1, CaV1.2))

Target
CaV1.x (where x specifies the subtype, e.g., CaV1.1, CaV1.2)
Molecular classification
Ion channel, Voltage-gated ion channel, Membrane protein
01

Overview

Voltage-gated calcium channel subunit alpha-1 proteins are transmembrane channels that open in response to changes in membrane potential, allowing the selective influx of calcium ions into cells. The L-type ("slow") calcium channels underlie the long-lasting calcium currents critical for muscle contraction, hormone and neurotransmitter secretion, and pacemaking in excitable tissues. They are heteromeric complexes but are defined by the pore-forming α1 subunit, which determines the channel's main properties and pharmacology. L-type channels are pharmacologically targeted by several classes of drugs (e.g., dihydropyridines, phenylalkylamines, benzothiazepines), with broad clinical use in cardiovascular and neurological conditions[5][4][3][1].

Other names
L-type calcium channelSlow calcium channelDihydropyridine-sensitive calcium channelCaV1.1 (skeletal muscle)CaV1.2 (cardiac, smooth muscle, neurons)CaV1.3CaV1.4 (retina)Slow inward channelVoltage-dependent calcium channel (VDCC)
02

Mechanism of action

Blockade of calcium influx by antagonizing the channel (calcium channel blockers) - Stabilization of the inactivated state (e.g., dihydropyridines)

03

Biological functions

Signal transductionExcitation-contraction coupling in muscleNeurotransmitter releaseGene expression regulationPacemaking activity in heart and neurons
04

Disease associations

Cardiovascular diseaseArrhythmiaHypertensionNeurological disordersEpilepsyMyopathy
05

Safety considerations

HypotensionBradycardiaEdemaCardiac conduction abnormalitiesNegative inotropic effects (reduced heart contractility)
06

Interacting drugs

Amlodipine

6 more in the full profile.

07

Biomarkers

Expression of CaV1.2 (CACNA1C) in cardiac tissue as a biomarker for cardiac disease riskGenetic variants in CACNA1C linked to susceptibility to arrhythmia and psychiatric disorders

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