Target intelligence / Profile preview

Voltage-gated calcium channel subunit alpha-1H (CaV3.2)

Target
CaV3.2
Molecular classification
Ion channel, Voltage-gated calcium channel, T-type calcium channel
01

Overview

Voltage-gated calcium channel subunit alpha-1H (CaV3.2) is a low-voltage-activated (T-type) calcium channel encoded by the CACNA1H gene, widely expressed in the central and peripheral nervous systems as well as heart and other tissues[1][3][5]. CaV3.2 channels conduct small, transient calcium influx at subthreshold membrane potentials, modulating neuronal excitability, pacemaker activity, neurotransmitter release, muscle contraction, cell proliferation, and apoptosis[4][5][6]. Dysfunction or dysregulation of CaV3.2 is associated with neurological diseases such as epilepsy, neuropathic pain, and potentially psychiatric and cardiovascular disorders[1][2][5]. CaV3.2 can be selectively blocked or modulated by certain small molecules or ions, making it a validated therapeutic target for pain, epilepsy, and related conditions[1][4][10]. Widespread physiological roles mean selective modulation and safety remain key challenges for drug development[5].

Other names
T-type calcium channel alpha-1H subunitCACNA1HCaV3.2Low-voltage-activated calcium channel alpha-1H subunitT-type Ca2+ channel
02

Mechanism of action

Channel blockade, leading to inhibition of low-voltage-activated calcium influx and reduced neuronal excitability Modulation of channel phosphorylation state to alter channel gating[2][5]

03

Biological functions

Signal transductionRegulation of neuronal excitabilityNeurotransmitter/hormone releasePacemaker activityMuscle contractionCell proliferationApoptosisGene expression
04

Disease associations

EpilepsyNeuropathic painNeuropsychiatric disordersCardiovascular diseaseCancerAutism spectrum disorders
05

Safety considerations

Off-target effects due to widespread expression in heart and brainCardiac conduction disturbances (since T-type channels modulate pacemaker activity)CNS depression and altered sensation/perception with systemic T-type channel blockers
06

Interacting drugs

Z944 (T-type calcium channel blocker; clinical trials for pain)

4 more in the full profile.

07

Biomarkers

CACNA1H overexpression/mutation as a genetic biomarker in familial epilepsy and certain pain syndromesCaV3.2 mRNA/protein levels in specific neuronal populations in preclinical studies

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