Picrotoxin (Synonyms: Cocculin；Picrotoxin；Picrotin ) |
| Catalog No.GC18511 |
Picrotoxin (Cocculin) is a plant alkaloid that is a non-competitive antagonist of GABAA receptors and can block the chloride channel of GABAA receptors.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 124-87-8
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
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.
| Cell experiment [1]: | |
|
Cell lines |
SCN cellls |
|
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. |
|
Reaction Conditions |
25, 50, 100, 500, and 1,000 µM; 4 days |
|
Applications |
Picrotoxin accelerates the circadian rhythm of neuronal firing activity in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
NG2-CreERTM:EYFP mice |
|
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. |
|
Dosage form |
1 mg/kg；i.p. |
|
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 | |
| Synonyms | Cocculin；Picrotoxin；Picrotin | ||
| Formula | C30H34O13 | M.Wt | 602.58 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 15 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *