CaV2.x Channels
CaV2.x channels are high-voltage activated calcium channels that are insensitive to blockade by dihydropyridines. There are three members in this family, which all show high expression in the central and peripheral nervous systems, where they mediate neurotransmitter release and are critical to neurotransmission.
CaV2.x Channel Activators |
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|---|---|
| Cat. No. | Product Name / Activity |
| 2851 | Nefiracetam |
| CaV1.x and CaV2.2 activator; cognitive enhancer | |
CaV2.x Channel Blockers |
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| Cat. No. | Product Name / Activity |
| 2799 | ω-Agatoxin IVA |
| CaV2.1 blocker | |
| 2802 | ω-Agatoxin TK |
| CaV2.1 blocker | |
| 2629 | Cilnidipine |
| Dual CaV1.x and CaV2.x blocker | |
| 1085 | ω-Conotoxin GVIA |
| CaV2.2 blocker | |
| 0840 | Loperamide hydrochloride |
| CaV1.x and CaV2.x blocker; also peripherally acting μ agonist | |
| 1439 | Ruthenium Red |
| Non-selective CaV2.1 and 2.2 blocker; also blocks TRPV channels | |
CaV2.x channels are high-voltage activated calcium channels that are insensitive to blockade by dihydropyridines. There are three members in this family, which all show high expression in the central and peripheral nervous systems, where they mediate neurotransmitter release and are critical to neurotransmission.
CaV2.1 channels (P/Q-type) may have a role in Alzheimer's disease, as amyloid-β oligomers are thought to directly regulate Ca2+ current through the channel. Mutations in the CaV2.1 α1-subunit have been linked to migraine headaches. Mutations in the CaV2.2 (N-type) α1-subunit have been associated with neuropsychiatric disorders including autism, bipolar disorder and schizophrenia. Selective blockers of CaV2.2 channels are used to treat chronic pain, via intrathecal injection into the spine. Few studies of CaV2.3 (R-type) channels have been reported to date.
External sources of pharmacological information for CaV2.x Channels :
Voltage-gated Calcium Channel Gene Data
| Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
|---|---|---|---|---|
| Cav2.1 | Human | CACNA1A | NM_000068 | Q99793 |
| Mouse | Cacna1a | NM_007578 | P97445 | |
| Rat | Cacna1a | NM_012918 | Q2YS39 | |
| Cav2.2 | Human | CACNA1B | NM_000718 | Q00975 |
| Mouse | Cacna1b | NM_007579 | O55017 | |
| Rat | Cacna1b | NM_147141 | Q9R1B6 | |
| Cav2.3 | Human | CACNA1E | NM_000721 | Q15878 |
| Mouse | Cacna1e | NM_009782 | Q61290 | |
| Rat | Cacna1e | NM_019294 | O35781 |