Table 1.
Clinically Used Drugs with Possible Neuroprotective Effects
| Drug | Pathways Inhibited | MW (g/mole) | Clinical Dose/mM | IC50 (mM)-T channel | Neuroprotective? |
|---|---|---|---|---|---|
| Anti-Epileptics | |||||
| Ethosuximide | T-Type (CaV3.1, CaV3.2); Na | 141.17 | 250-750mg PO BID/3.5-10 | 0.3-1.0 | Y |
| Trimethadione | T-Type (CaV3.2) | 143.14 | 300-600mg TID-QID/6-16.7 | ? | Y |
| Zonisamide | T-Type; Oxidative; Carbonic Anhydrase Inhibitor | 212.23 | 400-600mg qD/1.89-2.83 | 0.05-0.5 | Y |
| Anti-Hypertensives/Angina | |||||
| Amlodipine | T-Type (CaV3.2>CaV3.1 or CaV3.3) and L-Type; Na; K | 408.88 | 5-10mg qD/0.12-0.24 | 0.031 | Y |
| Aranidipine*J | T-Type and L-Type | 388.37 | 5-20mg qD/0.012-0.051 | 0.03-0.04 | ? |
| Azelnidipine*CJ | T-Type and L-Type | 582.65 | 8-16mg qD/0.014-0.028 | 0.04-0.07 | Y |
| Barnidipine*SJO | T-Type and L-Type | 528 | 10-15mg qD/0.019-0.028 | 0.005-0.02 | ? |
| Benidipine*IJCO | T-Type and L-Type | 542.02 | 2-4mg qD/0.0037-0.0074 | 0.003-0.2 | ? |
| Efonidipine*J | T-Type and L-Type | 631.66 | 40mg qD/0.63 | 0.0029 | ? |
| Mibefradil*O | T-Type and L-Type; Na; K | 568.55 | 400mg qD/0.70 | 0.00017-0.00029 | Y |
| Nicardipine | T-Type and L-Type | 515.99 | 20mg TID-120mg qD/0.11-0.23 | 0.0028 | Y |
| Nimodipine | T-Type and L-Type | 418.44 | 60mg q4h/0.86 | 0.0056 | Y |
| Other | |||||
| Lomerizine*J | T-Type and L-Type | 541.46 | 5-20mg qD/0.0009-0.0036 | 0.00000046 | Y |
| Pimozide | T-Type; Dopamine | 461.55 | 2-10mg BID/0.0089-0.043 | 0.000036-0.000054 | Y |
*
Not currently FDA approved; J= Japan, C= China, I= India, S= Spain, O= Other; MW = Molecular Weight