Picrotoxin
(Synonyms: 苦毒浆果[木防已属],Cocculin；Picrotoxin；Picrotin ) 目录号 : GC18511Picrotoxin(Cocculin)是一种植物生物碱,是 GABAA受体的非竞争性拮抗剂,可阻断GABAA受体的氯离子通道。
Cas No.:124-87-8
Sample solution is provided at 25 µL, 10mM.
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Picrotoxin (Cocculin) is a plant alkaloid that is a non-competitive antagonist of GABAA receptors and can block the chloride channel of GABAA receptors[1]. Picrotoxin does not act on the GABA recognition site, but may act on ion channels and can act as a central nervous system stimulant, causing excessive stimulation and convulsive reactions [2]. Picrotoxin is a non-competitive antagonist of glycine receptors [3].
In vitro, Picrotoxin (25-1000µM) treated SCN cells, concentration-dependently accelerated the circadian rhythm of cell discharge activity, and Picrotoxin (100µM) selectively advanced the accumulation of PER 2 protein by approximately 3.7 h without affecting PER 2 stability[4]. Picrotoxin (100µM) treated HEK293 cells, significantly inhibiting the expression of 5-HT3A receptors in the cells. Picrotoxin (10-300µM) inhibits 5-HT gated current in cells in a concentration-dependent manner, with an IC50 value of approximately 30µM[5].
In vivo, Picrotoxin (1mg/kg) treated NG2-CreERTM:EYFP mice via intraperitoneal injection for 5 days significantly increased the number and density of OPC neuron pairs[6]. Picrotoxin (2mg/kg) treated female CD rats by intraperitoneal injection increased the acetylcholine content in the striatum by approximately 70% and the level of homovanillic acid by approximately 30% [7].
References:
[1]Carpenter T S, Lau E Y, Lightstone F C. Identification of a possible secondary picrotoxin-binding site on the GABAA receptor[J]. Chemical research in toxicology, 2013, 26(10): 1444-1454.
[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]Qian H, Pan Y, Zhu Y, et al. Picrotoxin accelerates relaxation of GABAC receptors[J]. Molecular pharmacology, 2005, 67(2): 470-479.
[4]Freeman Jr G M, Nakajima M, Ueda H R, et al. Picrotoxin dramatically speeds the mammalian circadian clock independent of Cys-loop receptors[J]. Journal of neurophysiology, 2013, 110(1): 103-108.
[5]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.
[6]Boulanger J J, Messier C. Oligodendrocyte progenitor cells are paired with GABA neurons in the mouse dorsal cortex: Unbiased stereological analysis[J]. Neuroscience, 2017, 362: 127-140.
[7]Ladinsky H, Consolo S, Bianchi S, et al. Increase in striatal acetylcholine by picrotoxin in the rat: evidence for a gabergic-dopaminergic-cholinergic link[J]. Brain Research, 1976, 108(2): 351-361.
Picrotoxin(Cocculin)是一种植物生物碱,是 GABAA受体的非竞争性拮抗剂,可阻断GABAA受体的氯离子通道[1]。Picrotoxin不作用于GABA识别位点,但可能作用于离子通道内,可作为中枢神经系统兴奋剂,会引发过度刺激和惊厥反应[2]。Picrotoxin是甘氨酸受体的非竞争性拮抗剂[3]。
在体外,Picrotoxin(25-1000µM)处理SCN细胞,浓度依赖性地加速了细胞放电活动的昼夜节律,Picrotoxin(100µM)选择性地将PER 2蛋白的积累提前了约3.7 h,而不影响PER 2的稳定性[4]。Picrotoxin(100µM)处理HEK293细胞,显著抑制了细胞表达5-HT3A 受体。Picrotoxin(10-300µM)以浓度依赖性方式抑制细胞中5-HT门控电流,IC50值约为30µM[5]。
在体内,Picrotoxin(1mg/kg)通过腹腔注射处理NG2-CreERTM:EYFP小鼠5天,显著增加了OPC神经元对的数量和密度[6]。Picrotoxin(2mg/kg)通过腹腔注射处理雌性CD大鼠,使纹状体内乙酰胆碱含量增加约70%,高香草酸的水平增加约30%[7]。
| Cell experiment [1]: | |
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Cell lines |
SCN cellls |
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Preparation Method |
SCN cells were seeded on 30µm diameter electrodes and maintained in CO2 buffer for 3 weeks. Cover the culture chamber fixed to the array with fluorinated ethylene-polypropylene membrane and transfer to the recording incubator. Picrotoxin (25, 50, 100, 500, and 1,000 µM) was added to the culture and discharges sustained for at least 4 days were recorded for rhythmic analysis. |
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Reaction Conditions |
25, 50, 100, 500, and 1,000 µM; 4 days |
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Applications |
Picrotoxin accelerates the circadian rhythm of neuronal firing activity in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
NG2-CreERTM:EYFP mice |
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Preparation Method |
NG2-CreERTM:EYFP mice received i.p. injections of tamoxifen once a day for 5 days. On day 10, drinking water was replaced with sweetened water. On day 12, sweetened water was replaced with BrdU sweetened water. On days 13-17, mice received one injection per day of either saline, picrotoxin (1.0 mg/kg; n = 4). Mice were euthanized on day 75, 8 weeks following the end of BrdU exposure. |
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Dosage form |
1 mg/kg；i.p. |
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Applications |
Picrotoxin increased the number and density of OPC neuron pairs. |
|
References: [1] Freeman Jr G M, Nakajima M, Ueda H R, et al. Picrotoxin dramatically speeds the mammalian circadian clock independent of Cys-loop receptors[J]. Journal of neurophysiology, 2013, 110(1): 103-108. | |
| Cas No. | 124-87-8 | SDF | |
| 别名 | 苦毒浆果[木防已属],Cocculin；Picrotoxin；Picrotin | ||
| 分子式 | C30H34O13 | 分子量 | 602.58 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 15 mg/ml | 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 | 1.6595 mL | 8.2977 mL | 16.5953 mL |
| 5 mM | 0.3319 mL | 1.6595 mL | 3.3191 mL |
| 10 mM | 0.166 mL | 0.8298 mL | 1.6595 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >98.00%
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