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.
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.
Therapeutic Targets: epilepsy, pain sensing and cardiac pacemaking.
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.