Picrotoxinin是一种来源于天然植物的苦味毒素，存在于一种名为Anamirta cocculus的攀援植物的种子中，是一种氯离子通道阻断剂。Picrotoxinin是一种非竞争性的GABAA受体拮抗剂，负向调节神经递质γ氨基丁酸（GABA）对GABAA受体的作用。
Cas No.:17617-45-7
Sample solution is provided at 25 µL, 10mM.
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Picrotoxinin is a bitter toxin derived from natural plants; it is found in the seeds of a climbing plant known as Anamirta cocculus and acts as a chloride channel blocker[1, 2]. Picrotoxinin is a non-competitive antagonist of the GABAA receptor, negatively modulating the effects of the neurotransmitter gamma-aminobutyric acid (GABA) on GABAA receptors[3]. Picrotoxinin is a potent convulsant[4].
In vitro, treatment of Xenopus laevis oocytes with Picrotoxinin (0.001μM-1mM) for 90s inhibited GABA-induced chloride currents in a concentration-dependent manner; furthermore, it blocked the opening of chloride channels induced by various positive allosteric modulators (etomidate, propofol, diazepam, thiopentone sodium, loreclezole, and allopregnanolone)[5].
References:
[1] Katsnelson A. Making Natural Products Supernatural[J]. 2024.
[2] Olsen R W. Picrotoxin-like channel blockers of GABAA receptors[J]. Proceedings of the National Academy of Sciences, 2006, 103(16): 6081-6082.
[3] Das P, Bell-Horner C L, Machu T K, et al. The GABAA receptor antagonist picrotoxin inhibits 5-hydroxytryptamine type 3A receptors[J]. Neuropharmacology, 2003, 44(4): 431-438.
[4] Senghani M K, Patel P M, Sagar G V. Anticonvulsant activity of boswellic acids against maximal electroshock-induced convulsive rats and picrotoxin-induced convulsive mice[J]. Res J Pharmacon Phytochem, 2012, 4(6): 318-21.
[5] Ng C C, Duke R K, Hinton T, et al. Effects of bilobalide, ginkgolide B and picrotoxinin on GABAA receptor modulation by structurally diverse positive modulators[J]. European journal of pharmacology, 2017, 806: 83-90.
Picrotoxinin是一种来源于天然植物的苦味毒素，存在于一种名为Anamirta cocculus的攀援植物的种子中，是一种氯离子通道阻断剂[1, 2]。Picrotoxinin是一种非竞争性的GABAA受体拮抗剂，负向调节神经递质γ氨基丁酸（GABA）对GABAA受体的作用[3]。Picrotoxinin是一种有效的惊厥药[4]。
在体外，Picrotoxinin（0.001μM-1mM）处理非洲爪蟾卵母细胞90s，以浓度依赖性方式抑制了GABA诱导的氯离子电流，并且阻断了由各类正变构调节剂（etomidate, propofol, diazepam, thiopentone sodium, loreclezole, allopregnanoloner）所诱导的氯离子通道开放[5]。
| Cell experiment [1]: | |
| Cell lines | Xenopus laevis oocytes |
Preparation Method | Recordings were performed using the two-electrode voltage-clamp technique (holding potential: -60mV) in Xenopus laevis oocytes expressing recombinant human α1β2γ2L GABAA receptors. To evaluate the antagonistic effects of Picrotoxinin on positive allosteric modulators, experiments were conducted in two distinct modes: In the GABA-modulation mode, varying concentrations of Picrotoxinin (ranging from 0.001µM to 1mM) were co-incubated for 90s with 5µM GABA and the EC50 concentration of each respective positive modulator, in order to assess Picrotoxinin's ability to block the GABA-enhancing effect. In the GABA-mimetic mode, Picrotoxinin was co-incubated for 90s with the EC50 concentration of each positive modulator in the absence of GABA, to evaluate its inhibitory effect on the direct agonistic action of the positive modulators. A washout period of 3-5min was implemented after each drug application to prevent receptor desensitization and ensure the complete recovery of the baseline current. |
Reaction Conditions | 0.001µM-1mM; 90s |
Applications | Picrotoxinin inhibits GABA-induced chloride currents in a concentration-dependent manner, and concentration-dependently blocks the opening of chloride channels induced by GABA itself, as well as by various positive allosteric modulators. |
References: | |
| Cas No. | 17617-45-7 | SDF | |
| 别名 | 木防己苦毒宁 | ||
| Canonical SMILES | O=C1[C@]([C@@H]2C(C)=C)([H])[C@]3(O)C[C@]4([H])[C@](O4)(C(O5)=O)[C@]3(C)[C@@]5([H])[C@]2([H])O1 | ||
| 分子式 | C15H16O6 | 分子量 | 292.28 |
| 溶解度 | DMSO : 100 mg/mL (342.14 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4214 mL | 17.1069 mL | 34.2138 mL |
| 5 mM | 684.3 μL | 3.4214 mL | 6.8428 mL |
| 10 mM | 342.1 μL | 1.7107 mL | 3.4214 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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