|
Potent, selective L-type voltage gated calcium channel blocker; antihypertensive
Prod. No. I6658
Voltage-gated calcium channels are a major route of calcium translocation across the plasma membrane of excitable cells. Six types of calcium channels have been identified: T, L, N, P, Q, and R. T-type channels need only small depolarizations to be activated (low-voltage activated, LVA), while the other types require larger depolarizations (high-voltage activated, HVA). Compounds such as verapamil, isradipine, nefedipine, dilantizem and 1,4-dihydropine analogs of nefedipine interact with the L-type calcium channel and are widely used as antihypertensives and in the treatment of certain vascular disorders.
Features & Benefits
Isradipine has been widely used in the study of hypertension, ischemia, and depression. It belongs to the class of compounds known as 1,4 dihydropyridines, and appears to be selective for the L-type calcium channel subtype CaV1.2 (1).
- Isradipine (2.5 mg/kg) significantly reduced the volume of ischemic brain damage in the cerebral hemisphere (25%; P = 0.0001), cerebral cortex (18%; P = 0.0034), and caudate nucleus (33%; P = 0.0002) in spontaneously hypertensive rats when assessed at 24 h post-MCA occlusion (2).
- Isradipine, as well as several other DHP drugs (nicardipine, nitrendipine, felodipine, nimodipine) displayed antidepressant-like properties in the tail suspension test in mice (3).
- Isradipine-induced acceleration of the CaV1.2 current decay may reflect enhanced fast voltage-dependent inactivation rather than open channel block in a calcium channel construct Lh, corresponding to rabbit cardiac α1C-a cDNA (1).
| Additional L-type calcium channel blockers offered by Sigma-RBI |
|
| Product Name |
Product # |
| (R)-(+)-Bay K8644 Manufactured and sold with the permission of Bayer AG |
B-132 |
| Calcicludine 2 |
C2836 |
| Dilantizem |
D2521 |
| Felodipine |
F9677 |
| FS-2 |
F3176 |
| Nicardipine |
N7510 |
| Nifedipine |
N7634 |
| Nimodipine |
N-149 |
| Nitrendipine |
N-144 |
| S-Petasin |
P4243 |
| Phloretin |
P7912 |
| (+)-Verapamil hydrochloride |
V4629 |
References
- Berjukow, S and Hering, S. Voltage-dependent acceleration of Cav1.2 channel current decay by (+)- and (-)- isradipine. Br. J. Pharmacol., 133, 959-966, 2001.
- Campbell, C.A., et al., Effects of isradipine, an L-type calcium channel blocker on permanent and transient focal cerebral ischemia in spontaneously hypertensive rats. Exp. Neurol., 148, 45-50, 1997.
- Cohen, C., et al., Assessment of the antidepressant-like effects of L-type voltage-dependent channel modulators. Behav. Pharmacol., 8, 629-638, 1997.
For more information about calcium channel modulators, please visit The Sigma-RBI Handbook of Receptor Classification and Signal Transduction.
back to top
|
