Voltage-gated Sodium (NaV) Channels
Voltage-gated sodium channels (NaV) are responsible for action potential initiation and propagation in excitable cells, including nerve, muscle, and neuroendocrine cell types. They are also expressed at low levels in non-excitable cells, where their physiological role is unclear.
Activators |
|
|---|---|
| Cat No | Product Name / Activity |
| 5941 | OD1 |
| Potent hNav1.4, rNav1.6 and rNav1.7 channel activator | |
| 2918 | Veratridine |
| Voltage-gated Na+ channel opener | |
Blockers |
|
| Cat No | Product Name / Activity |
| 2976 | A 803467 |
| Selective NaV1.8 channel blocker | |
| 4249 | A 887826 |
| Potent voltage-dependent NaV1.8 channel blocker | |
| 2404 | Ambroxol hydrochloride |
| Na+ channel blocker | |
| 0890 | Amiloride hydrochloride |
| Na+ channel blocker; also I2 imidazoline ligand | |
| 6159 | 4,9-Anhydrotetrodotoxin |
| Potent and selective Nav1.6 channel blocker | |
| 4804 | APETx2 |
| NaV1.8 and NaV1.2 blocker; also blocks ASIC3 channels | |
| 4098 | Carbamazepine |
| Inhibitor of neuronal voltage-gated Na+ channels; anticonvulsant | |
| 2642 | Co 102862 |
| State-dependent of voltage-gated sodium channels | |
| 1470 | Flecainide acetate |
| Cardiac Na+ channel blocker. Antiarrhythmic | |
| 0522 | Flunarizine dihydrochloride |
| Dual Na+/Ca2+ channel (T-type) blocker | |
| 4718 | Huwentoxin IV |
| Selective NaV1.7 channel blocker | |
| 5066 | ICA 121431 |
| Potent and selective NaV1.3 and NaV1.1 channel blocker | |
| 4913 | Jingzhaotoxin III |
| Selective NaV1.5 channel blocker | |
| 3251 | KC 12291 hydrochloride |
| Orally active atypical Na+ channel blocker; cardioprotective | |
| 3865 | Licarbazepine |
| Active metabolite of oxcarbazepine (Cat. No. 3864) | |
| 3057 | Lidocaine |
| Na+ channel blocker | |
| 2596 | Mexiletine hydrochloride |
| Na+ channel blocker; antiarrhythmic agent | |
| 4691 | NAV 26 |
| Selective Nav1.7 channel blocker | |
| 3864 | Oxcarbazepine |
| Anticonvulsant; inhibits Na+ channel activity | |
| 4916 | PF 04885614 |
| Potent and selective NaV1.8 channel blocker; active in vivo | |
| 5931 | PF 05089771 |
| Potent and selective Nav1.7 channel blocker | |
| 4914 | Phrixotoxin 3 |
| Potent blocker of NaV1.2, NaV1.3 and NaV1.5 channels | |
| 4665 | ProTx I |
| CaV3.1 channel blocker; also inhibits NaV1.8 and KV2.1 | |
| 4023 | ProTx II |
| Selective NaV1.7 channel blocker | |
| 5792 | ProTx III |
| Potent Nav1.7 blocker; analgesic | |
| 1043 | QX 222 |
| Na+ channel blocker | |
| 1014 | QX 314 bromide |
| Na+ channel blocker | |
| 2313 | QX 314 chloride |
| Na+ channel blocker | |
| 4029 | Ralfinamide mesylate |
| Na+ channel blocker | |
| 0768 | Riluzole hydrochloride |
| Na+ channel blocker | |
| 4044 | Sipatrigine |
| NaV blocker; neuroprotective | |
| 4435 | TC-N 1752 |
| NaV channel blocker | |
| 1078 | Tetrodotoxin |
| Na+ channel blocker | |
| 1069 | Tetrodotoxin citrate |
| Na+ channel blocker; citrate salt of tetrodotoxin (Cat. No. 1078) | |
| 2815 | Valproic acid, sodium salt |
| Blocks voltage-gated Na+ channels | |
| 0757 | Vinpocetine |
| Na+ channel blocker | |
Other |
|
| Cat No | Product Name / Activity |
| 5184 | BDS I |
| Attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels; neuroprotective | |
| 1539 | β-Pompilidotoxin |
| Slows neuronal Na+ channel inactivation | |
| 5470 | QAQ dichloride |
| Photoswitchable Nav, Kv and Cav channel blocker | |
| 3828 | Rufinamide |
| Prolongs inactivation of sodium channels; anticonvulsant | |
Voltage-gated sodium channels (NaV) are responsible for action potential initiation and propagation in excitable cells, including nerve, muscle, and neuroendocrine cell types. They are also expressed at low levels in non-excitable cells, where their physiological role is unclear.
Structurally, NaV channels are composed of one pore-forming α-subunit, which may be associated with either one or more β-subunits. α-subunits are composed for four homologous domains, each of which contains six transmembrane segments. The fourth transmembrane loop (S4) acts as the 'voltage sensor' and is activated by changes in membrane potential. S4 is also involved in channel gating.
External sources of pharmacological information for Voltage-gated Sodium (NaV) Channels :
Literature for Voltage-gated Sodium (NaV) Channels
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Voltage-gated Sodium Channel Gene Data
| Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
|---|---|---|---|---|
| NaV1.1 | Human | SCN1A | NM_006920 | P35498 |
| Mouse | Scn1a | NM_018733 | NP_061203 | |
| Rat | Scn1a | NM_030875 | P04774 | |
| NaV1.2 | Human | SCN2A | NM_021007 | Q99250 |
| Mouse | Scn2a1 | NM_001099298 | NP_001092768 | |
| Rat | Scn2a1 | NM_012647 | P04775 | |
| NaV1.3 | Human | SCN3A | NM_006922 | Q9NY46 |
| Mouse | Scn3a | NM_018732 | NP_061202 | |
| Rat | Scn3a | NM_013119 | P08104 | |
| NaV1.4 | Human | SCN4A | NM_000334 | P35499 |
| Mouse | Scn4a | NM_133199 | NP_573462 | |
| Rat | Scn4a | NM_013178 | P15390 | |
| NaV1.5 | Human | SCN5A | NM_198056 | Q14524 |
| Mouse | Scn5a | NM_021544 | NP_067519 | |
| Rat | Scn5a | NM_013125 | P15389 | |
| NaV1.6 | Human | SCN8A | NM_014191 | Q9UQD0 |
| Mouse | Scn8a | NM_001077499 | Q9WTU3 | |
| Rat | Scn8a | NM_019266 | O88420 | |
| NaV1.7 | Human | SCN9A | NM_002977 | Q15858 |
| Mouse | Scn9a | NM_018852 | Q62205 | |
| Rat | Scn9a | NM_133289 | O08562 | |
| NaV1.8 | Human | SCN10A | NM_006514 | Q9Y5Y9 |
| Mouse | Scn10a | NM_009134 | Q6QIY3 | |
| Rat | Scn10a | NM_017247 | Q62968 | |
| NaV1.9 | Human | SCN11A | NM_014139 | Q9UI33 |
| Mouse | Scn11a | NM_011887 | Q9R053 | |
| Rat | Scn11a | NM_019265 | O88457 | |
| β1 | Human | SCN1B | NM_001037 | Q07699 |
| Mouse | Scn1b | NM_011322 | P97952 | |
| Rat | Scn1b | NM_017288 | Q00954 | |
| β2 | Human | SCN2B | NM_004588 | O60939 |
| Mouse | Scn2b | NM_001014761 | Q56A07 | |
| Rat | Scn2b | NM_012877 | P54900 | |
| β3 | Human | SCN3B | NM_018400 | Q9NY72 |
| Mouse | Scn3b | NM_153522 | Q8BHK2 | |
| Rat | Scn3b | NM_139097 | Q9JK00 | |
| β4 | Human | SCN4B | NM_174934 | Q8IWT1 |
| Mouse | Scn4b | NM_001013390 | Q7M729 | |
| Rat | Scn4b | NM_001008880 | Q7M730 |
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