Voltage-gated calcium channels (VGCC) are found in excitable cells such as muscle and neurons. There are various voltage-gated calcium channel α1 subtypes

• L-type (Cav1.1, 1.2, 1.3, 1.4) channels

• P/Q-type (Cav2.1) channels

• N-type (Cav2.2) channels

• R-type (Cav2.3) channels

• T-type (Cav3.1, 3.2. 3.3) channels

Fig.1 Diagram of voltage-gated calcium channel subunit topology

Calcium channel have been well recognized as therapeutic targets for treating a number of diseases. However, the calcium channel class is considered to be underexploited due to the lack of reliable functional cell-based assays for high-throughput screening.

Fig. 2 The most important physiologic functions of the different LTCC isoforms

Here, Creative Bioarray utilizes automated patch-clamp technique to test various calcium channel activities with your compound treatment and digital cell Ca²⁺ imaging with fura-2 AM dye in single human living cells (primary cultured cells or stable-expressing cell lines). We also offer [Ca²⁺]i measurement to test effects of lead compounds on GPCR-mediated [Ca²⁺]i signaling pathway, such as Ca-sensing receptor and other GPCR.

Voltage-gated Calcium channels

Cav1.2/β2/α2δ1 (CACNA1C/CACNB2/CACNA2D1)

Tissue Specific Expression: heart, smooth muscle, neurons and endocrine tissue.

Therapeutic Targets: cardiac arrhythmia and hypertension.

Cav2.1/β3/α2δ2 (CACNA1A/CACNB3/CACNA2D2 or CACNA2D4)

Disease: mutations in CACNA1A are responsible for several inherited neurologic disorders including familial hemiplegic migraine, episodic ataxia type 2, and spinocerebellar ataxia type 6 epilepsy.

Therapeutic Targets: pain management.

Cav3.1 (CACNA1G)

Therapeutic Targets: epilepsy, pain sensing and cardiac pacemaking.

Cav3.2 (CACNA1H)

Disease: mutations in CACNA1H have been linked to inherited neurologic diseases including idiopathic, generalized and childhood absence epilepsies.

Therapeutic Targets: seizures, hypertension, angina, neuropathic pain, insomnia, and cancer.

Reference

1. Zamponi GW, et al. The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential. Pharmacol Rev. 2015; 67: 821–870.

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