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  • ω-Conotoxin GVIA
ω-Conotoxin GVIA的可视化放大

ω-Conotoxin GVIA

ω-芋螺毒素 GVIA 是 N 型 Ca2+ 通道的抑制剂。

原价
¥3875-3875
价格
3100-3100
ω-Conotoxin GVIA的二维码

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  • 货号: ajci12014
  • CAS: 106375-28-4
  • 别名: Ω-芋螺毒素
  • 分子式: C120H182N38O43S6
  • 分子量: 3037.35
  • 纯度: >98%
  • 溶解度: Soluble to 1 mg/ml in Water
  • 储存: Desiccate at -20°C
  • 库存: 现货

Background

ω-Conotoxin GVIA is a cone snail toxin that selectively blocks N-type channels in neurons [1].


ω-Conotoxin GVIA binds to human neocortical, rat hippocampal, and chick brain synaptic plasma membranes (IC50s = 4.6, 60, and 150 pM, respectively, in radioligand binding assays) [3,4,5].


ω-Conotoxin GVIA markedly reduced the amplitude of the tetanic contractions of the tibialis anterior muscle in mice, but tetanic facilitation was not impaired. The muscle contractions elicited by direct electrical stimulation were not significantly modified by ω-Conotoxin GVIA. ω-Conotoxin GVIA did not had any significant changes in systemic blood pressure [5].

参考文献:
[1]. H.D. Mansvelder, J.C. Stoof, K.S. Kits. Dihydropyridine block of ω-agatoxin IVA- and ω-conotoxin GVIA-sensitive Ca2+ channels in rat pituitary melanotropic cells.Eur. J. Pharmacol., 311 (1996), pp. 293-304
[2]. Feuerstein, T.J., Dooley, D.J., and Seeger, W. Inhibition of norepinephrine and acetylcholine release from human neocortex by ω-conotoxin GVIA. J. Pharmacol. Exp. Ther. 252(2), 778-785 (1990).
[3]. Lampe, R.A., Lo, M.M., Keith, R.A., et al. Effects of site-specific acetylation on ω-conotoxin GVIA binding and function. Biochemistry 32(13), 3255-3260 (1993).
[4]. Sato, K., Park, N.G., Kohno, T., et al. Role of basic residues for the binding of ω-conotoxin GVIA to N-type calcium channels. Biochem. Biophys. Res. Commun. 194(3), 1292-1296 (1993).
[5]: Rossoni G, Berti F, La Maestra L, Clementi F. ω-Conotoxin GVIA binds to and blocks rat neuromuscular junction. Neuroscience Letters. 1994;176:185-188.


ω-芋螺毒素 GVIA 是一种锥形蜗牛毒素,可选择性地阻断神经元中的 N 型通道[1]


ω-芋螺毒素 GVIA 与人类新皮质、大鼠海马和鸡脑突触质膜结合(在放射性配体结合试验中,IC50 分别 = 4.6、60 和 150 pM)[3,4,5].


ω-芋螺毒素 GVIA 显着降低了小鼠胫骨前肌的强直收缩幅度,但强直易化作用并未受损。 ω-芋螺毒素 GVIA 未显着改变由直接电刺激引起的肌肉收缩。 ω-芋螺毒素 GVIA 对体循环血压无明显影响[5]

Protocol

Cell experiment [1]:

Cell lines

Rat pituitary melanotropic cells

Preparation Method


Reaction Conditions

1 or 10 μM

Applications

1 μM ω-Conotoxin GVIA blocked the high voltage-activated current by 25.5±3.6%. The block at 10μM ω-Conotoxin GVIA was 22.9±2.5% (not significantly different from the block by 1μM;n = 3), indicating thatω-Conotoxin GVIA yields a saturating effect.

Animal experiment [2]:

Animal models

male COBS CD (SD) rats

Preparation Method

In these animals the intravenous administration of graded doses of ω-Conotoxin GVIA (1--2 nmol/kg)

Dosage form

Intravenous injection, 1--2 nmol/kg

Applications

Intravenous injection caused a progressive loss of tension development of tibialis muscle indirectly evoked by the electrical stimulation of the sciatic nerve, ω-Conotoxin GVIA (1 nmol/kg i.v.) reduced the strength of muscle contraction by 75% in about 27 min (from

参考文献:

[1]: H.D. Mansvelder, J.C. Stoof, K.S. Kits. Dihydropyridine block of ω-agatoxin IVA- and ω-conotoxin GVIA-sensitive Ca2+ channels in rat pituitary melanotropic cells.Eur. J. Pharmacol., 311 (1996), pp. 293-304
[2]: Rossoni G, Berti F, La Maestra L, Clementi F. ω-Conotoxin GVIA binds to and blocks rat neuromuscular junction. Neuroscience Letters. 1994;176:185-188.

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