Target intelligence / Profile preview

L-type and T-type calcium channel

Molecular classification
Ion channel, Voltage-gated ion channel
01

Overview

L-type and T-type calcium channels are two distinct classes of voltage-gated calcium channels widely expressed in cardiac, vascular smooth muscle, and neural tissues. L-type calcium channels, primarily the Cav1.2 isoform, are high-voltage activated channels that mediate calcium influx in response to membrane depolarization, triggering smooth muscle contraction, heart muscle contractility, and hormone secretion. T-type calcium channels, including the Cav3.1, Cav3.2, and Cav3.3 isoforms, activate at lower voltages and inactivate rapidly, contributing to pacemaking activity, neuronal firing, and modulation of vascular tone. Both channel types play critical roles in excitation-contraction coupling, regulation of vascular resistance, heart rhythm, and cellular proliferation. Numerous calcium channel blockers target L-type channels for hypertension and cardiac disease, while T-type selective inhibitors like mibefradil (now withdrawn) have been explored for arrhythmias and neurological disorders. Channel dysfunction or dysregulation is implicated in cardiovascular, neurological, and proliferative diseases.

Other names
Voltage-gated calcium channel (Cav1 and Cav3 families)Cav1.2 (L-type)Cav3.1/Cav3.2/Cav3.3 (T-type)Voltage-dependent calcium channel
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Mechanism of action

Inhibition of calcium influx during membrane depolarization to reduce muscle contraction, vascular tone, or pacemaker activity; Stabilization of cell membrane potential by reducing T-type channel opening

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Biological functions

Excitation-contraction couplingSignal transductionRegulation of vascular tonePacemaking activity in the heartCell proliferationNeurotransmitter release
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Disease associations

Cardiovascular diseaseHypertensionArrhythmiasNeurological diseases (e.g., epilepsy, pain, Parkinson’s disease)CancerOther (role in tissue remodeling and cell growth)
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Safety considerations

HypotensionBradycardia/arrhythmiaRisk of worsening heart failure (L-type blockers)CNS depression, dizzinessPotential off-target effects on cardiac conduction system
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Interacting drugs

Verapamil (L-type selective calcium channel blocker)

6 more in the full profile.

07

Biomarkers

Expression levels of Cav1.2 (CACNA1C) and Cav3.x subunits (CACNA1G, CACNA1H, CACNA1I) in tissueFunctional assays of voltage-gated calcium current

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