w-Conotoxin MVIIA
- 貨號 Cat. No.
- C-670
- 規格 Size
- 50 μg 5x50 μg 0.1mg 5x0.1mg 0.1mg
Description
w-Conotoxin MVIIA
Specific Cav2.2 Channel Blocker
| Product#: | C-670 |
| Sizes: |
| 50 mg |
| 5 x 50 mg |
| 0.1 mg |
| 5 x 0.1 mg |
| M.W.: | 2639 |
| Sequence: | CKGKG AKCSR LMYDC CTGSC RSGKC |
| Purity: | >99% |
| Bioassay: |
Inhibition of Cav2.2 channels expressed in Xenopus oocytes using different concentrations of w-Conotoxin MVIIA. Left: Time course of amplitude change upon application of w-Conotoxin MVIIA (C-670). Times of toxin application at the indicated concentrations are denoted with arrows. Right: Example traces before or during perfusion of 200 nM toxin. |
 |
| References: |
1. | Olivera, B.M. et al. (1987) Biochemistry 26, 2086. |
2. | Luchian, T. (2001) Biochim. Biophys. Acta. 1512, 329. |
3. | Stocker, J.W. et al. (1997) J. Neurosci 17, 3002. |
4. | Newcomb, R. et al. (1994) Brain. Res. 638, 95. |
5. | Vega, T. et al. (1995) Eur. J. Pharmacol. 276, 231. |
6. | Hirata, H. et al. (1997) Eur. J. Pharmacol. 321, 217. |
7. | Sanger, G.J. et al. (2000) Eur. J. Pharmacol. 388, 89. |
8. | Stoehr, S.J. et al. (1993) Neurosci. Lett. 161, 113. |
9. | Feng, Z.P. et al. (2001) J. Biol. Chem. 276, 15278. |
w-Conotoxin MVIIA is a synthetic peptidyl toxin originally isolated from Conus magus snail venom. w-Conotoxin MVIIA, specifically blocks Cav2.2 (a1B, N-type) channels1. The effect of the toxin is modulated by Cavb auxiliary subunit2 and by voltage (i.e. it is more potent for inactivated channels)3.
w-Conotoxin MVIIA inhibits K+-induced 3H-GABA release in hippocampus in vivo4. This effect was with high affinity (50% block, 200 nM). The toxin was used to inhibit synaptic transmission in several peripheral preparations5, 6, 7. The toxin binds with high affinity to rat neocortical membranes8. It blocked cloned Cav2.2 channels transiently expressed in tsa-2019 and in Xenopus oocytes3.
The FDA recently approved Prialt (synthetic w-Conotoxin MVIIA) to treat severe chronic pain in patients who are intolerant of or refractory to other treatments such as systemic analgesics or morphine. This is the first ion channel blocker to be marketed for pain.
The FDA recently approved Prialt (synthetic w-Conotoxin MVIIA) to treat severe chronic pain in patients who are intolerant of or refractory to other treatments such as systemic analgesics or morphine. This is the first ion channel blocker to be marketed for pain.