CaV1.x Channels (L-type)

CaV1.x channels (L-type) are high-voltage activated Ca2+ channels that are sensitive to blockade by dihydropyridines. This family has four members, each composed of an α1, α2/δ, β and γ subunit. Mutations in the α1-subunit of CaV1.x channels have been linked to various cardiac arrhythmias and neuropsychiatric diseases.

Products
Background
Literature
Gene Data

Activators

Cat. No. Product Name / Activity
1544 (±)-Bay K 8644
CaV1.x activator
1546 (S)-(-)-Bay K 8644
CaV1.x activator; (S)-(-)-enantiomer of (±)-Bay K 8644
1403 FPL 64176
Potent CaV1.x activator
2851 Nefiracetam
CaV1.x and CaV2.2 activator; cognitive enhancer

Blockers

Cat. No. Product Name / Activity
2571 Amlodipine besylate
CaV1.x blocker
1545 (R)-(+)-Bay K 8644
CaV1.x blocker; (R)-(+)-enantiomer of (±)-Bay K 8644
2629 Cilnidipine
Dual CaV1.x and CaV2.x blocker
6170 Cinacalcet hydrochloride
CaV1.x blocker; also CaSR allosteric agonist and CYP2D2 inhibitor
0685 Diltiazem hydrochloride
CaV1.x blocker
3733 Efonidipine hydrochloride monoethanolate
CaV1.x and CaV3.x blocker
2960 Felodipine
CaV1.x blocker
6407 Fendiline Hydrochloride
CaV1.x blocker; also K-Ras inhibitor
2004 Isradipine
CaV1.x blocker
2959 Lercanidipine hydrochloride
CaV1.x blocker
0840 Loperamide hydrochloride
CaV1.x and CaV2.x blocker; also peripherally acting μ agonist
1075 Nifedipine
CaV1.x blocker
1124 (R)-(-)-Niguldipine hydrochloride
CaV1.x blocker; also α1A antagonist; less active enantiomer of (S)-(+)-Niguldipine
1123 (S)-(+)-Niguldipine hydrochloride
CaV1.x blocker; also α1A antagonist
5711 Nilvadipine
CaV1.x blocker; also Syk kinase inhibitor
0600 Nimodipine
CaV1.x blocker
0601 Nitrendipine
CaV1.x blocker
1806 SR 33805 oxalate
CaV1.x blocker; binds allosterically to distinct site
0654 Verapamil hydrochloride
CaV1.x blocker

CaV1.x channels (L-type) are high-voltage activated Ca2+ channels that are sensitive to blockade by dihydropyridines. This family has four members, each composed of an α1, α2/δ, β and γ subunit.

CaV1.1 channels are specific to skeletal muscle where they interact with ryanodine receptors on the sarcoplasmic reticulum and trigger Ca2+ influx, Ca2+-activated Ca2+ release and muscle contraction. Mutations in CaV1.1 α1-subunit have been linked to hypokalemic periodic paralysis.

CaV1.2 and 1.3 channels are found in most excitable cells. In the brain, they are located postsynaptically, where they modulate neuronal firing and Ca2+-coupled gene transcription. By supporting neuronal plasticity, these channels are critical to processes such as learning and memory, addiction and neural development. As well as being found in the brain, CaV1.2 and 1.3 channels are found in the heart. CaV1.2 are the predominant subtype in cardiomyocytes, where they trigger contraction, however they are also found in smaller numbers in sinoatrial and atrioventricular node cells. CaV1.3 are the predominant subtype in these cells, and CaV1.2 and 1.3 channels play roles at different stages of the cardiac action potential. Additionally, CaV1.2 and 1.3 channels are found in endocrine cells; CaV1.2 control the fast phase of insulin secretion in mouse pancreatic β-cells, while CaV1.3 are required for β-cell proliferation and development. Mutations in the CaV1.2 α1-subunit have been linked to various cardiac arrhythmias, as well as neuropsychiatric diseases including autism. Similarly, mutations in CaV1.3 α1-subunit have been linked to autism, and also Parkinson's disease.

CaV1.4 channels are mainly restricted to the retina, where they are essential for normal visual function; congenital stationary night blindness has been linked to mutations in CaV1.4 channels.

External sources of pharmacological information for CaV1.x Channels (L-type) :

    Literature for CaV1.x Channels (L-type)

    Tocris offers the following scientific literature for CaV1.x Channels (L-type) to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


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    Cav1.x Voltage-gated Calcium Channel Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Cav1.1 Human CACNA1S NM_000069 Q13698
    Mouse Cacna1s NM_001081023 Q02789
    Rat Cacna1s NM_053873 Q02485
    Cav1.2 Human CACNA1C NM_000719 Q6PKM7
    Mouse Cacna1c NM_009781 Q01815
    Rat Cacna1c NM_012517 Q8VHT3
    Cav1.3 Human CACNA1D NM_000720 Q01668
    Mouse Cacna1d NM_001083616 Q99246
    Rat Cacna1d NM_017298 Q91XN9
    Cav1.4 Human CACNA1F NM_005183 O60840
    Mouse Cacna1f NM_019582 Q9JIS7
    Rat Cacna1f NM_053701 Q923Z7