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Voltage-gated calcium channels (CaV) C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Ca2+ channels are voltage-gated ion channels present in the membrane of most excitable cells. The nomenclature for Ca2+channels was proposed by [9] and approved by the NC-IUPHAR Subcommittee on Ca2+ channels [6]. Most Ca2+ channels form hetero-oligomeric complexes. The α1 subunit is pore-forming and provides the binding site(s) for practically all agonists and antagonists. The 10 cloned α1-subunits can be grouped into three families: (1) the high-voltage activated dihydropyridine-sensitive (L-type, CaV1.x) channels; (2) the high- to moderate-voltage activated dihydropyridine-insensitive (CaV2.x) channels and (3) the low-voltage-activated (T-type, CaV3.x) channels. Each α1 subunit has four homologous repeats (I-IV), each repeat having six transmembrane domains (S1-S6) and a pore-forming region between S5 and S6. Voltage-dependent gating is driven by the membrane spanning S4 segment, which contains highly conserved positive charges that respond to changes in membrane potential. All of the α1-subunit genes give rise to alternatively spliced products. At least for high-voltage activated channels, it is likely that native channels comprise co-assemblies of α1, β and α2-δ subunits. The γ subunits have not been proven to associate with channels other than the α1s skeletal muscle Cav1.1 channel. The α2-δ1 and α2-δ2 subunits bind gabapentin and pregabalin.

Channels and Subunits

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Targets of relevance to immunopharmacology are highlighted in blue

Cav1.1 C Show summary » More detailed page go icon to follow link

Cav1.2 C Show summary » More detailed page go icon to follow link

Cav1.3 C Show summary » More detailed page go icon to follow link

Cav1.4 C Show summary » More detailed page go icon to follow link

Cav2.1 C Show summary » More detailed page go icon to follow link

Cav2.2 C Show summary » More detailed page go icon to follow link

Cav2.3 C Show summary » More detailed page go icon to follow link

Cav3.1 C Show summary » More detailed page go icon to follow link

Cav3.2 C Show summary » More detailed page go icon to follow link

Cav3.3 C Show summary » More detailed page go icon to follow link

Further reading

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Mathie AA, Peters JA, Veale EL, Striessnig J, Kelly E, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Ion channels. Br J Pharmacol. 180 Suppl 2:S145-S222.