Date published: 2025-11-3

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Picrotoxin (CAS 124-87-8)

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Alternate Names:
Cocculin
Application:
Picrotoxin is a GABAA receptor antagonist
CAS Number:
124-87-8
Molecular Weight:
602.58
Molecular Formula:
C15H18O7•C15H16O6
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Picrotoxin is a GABAA receptor antagonist, often utilized in neurophysiological research to study the inhibitory neurotransmission mediated by GABA. It binds to the GABAA receptor chloride channel, blocking the flow of chloride ions and thus inhibiting the hyperpolarizing effect of GABA on neurons. This action is useful in experimental applications for probing the dynamics of neuronal excitability and for inducing a controlled state of increased neuronal firing. Research involving picrotoxin also helps in delineating the role of inhibitory synapses in various neural circuits and in the overall regulation of brain activity. Additionally, this compound is instrumental in electrophysiological studies, where it is used to understand the contribution of GABAergic inhibition to phenomena such as oscillatory behavior and synaptic plasticity within neural networks.


Picrotoxin (CAS 124-87-8) References

  1. Picrotoxin increased acetylcholine release from rat cultured embryonic septal neurons.  |  Suzuki, T., et al. 2004. Neurosci Lett. 356: 57-60. PMID: 14746901
  2. Picrotoxin accelerates relaxation of GABAC receptors.  |  Qian, H., et al. 2005. Mol Pharmacol. 67: 470-9. PMID: 15509715
  3. Picrotoxin inhibition mechanism of a gamma-aminobutyric acid A receptor investigated by a laser-pulse photolysis technique.  |  Ramakrishnan, L. and Hess, GP. 2005. Biochemistry. 44: 8523-32. PMID: 15938643
  4. A picrotoxin-specific conformational change in the glycine receptor M2-M3 loop.  |  Hawthorne, R. and Lynch, JW. 2005. J Biol Chem. 280: 35836-43. PMID: 16109711
  5. Neuroendocrine, behavioral and macrophage activity changes induced by picrotoxin effects in mice.  |  Stankevicius, D., et al. 2008. Neuropharmacology. 54: 300-8. PMID: 18022650
  6. Stability of picrotoxin during yogurt manufacture and storage.  |  Jablonski, JE. and Jackson, LS. 2008. J Food Sci. 73: T121-8. PMID: 19019133
  7. Administration of the GABAA receptor antagonist picrotoxin into rat supramammillary nucleus induces c-Fos in reward-related brain structures. Supramammillary picrotoxin and c-Fos expression.  |  Shin, R. and Ikemoto, S. 2010. BMC Neurosci. 11: 101. PMID: 20716371
  8. Picrotoxin but not bicuculline partially abolishes the cardio-inhibitory responses induced by visual stimulation in the crab Neohelice granulata.  |  Yang, M., et al. 2013. Physiol Behav. 110-111: 198-205. PMID: 23283252
  9. Picrotoxin dramatically speeds the mammalian circadian clock independent of Cys-loop receptors.  |  Freeman, GM., et al. 2013. J Neurophysiol. 110: 103-8. PMID: 23576702
  10. Identification of a possible secondary picrotoxin-binding site on the GABA(A) receptor.  |  Carpenter, TS., et al. 2013. Chem Res Toxicol. 26: 1444-54. PMID: 24028067
  11. Effects of picrotoxin treatment on GABAA receptor supramolecular complexes in rat brain.  |  Ito, Y., et al. 1989. J Neurochem. 52: 1064-70. PMID: 2538560
  12. Bicuculline and picrotoxin block gamma-aminobutyric acid-gated Cl- conductance by different mechanisms.  |  Akaike, N., et al. 1985. Experientia. 41: 70-1. PMID: 2578409
  13. GABAA receptor signalling mechanisms revealed by structural pharmacology.  |  Masiulis, S., et al. 2019. Nature. 565: 454-459. PMID: 30602790
  14. Pharmacology of novel GABA receptors found on rod horizontal cells of the white perch retina.  |  Qian, H. and Dowling, JE. 1994. J Neurosci. 14: 4299-307. PMID: 8027780
  15. Multiple mechanisms of picrotoxin block of GABA-induced currents in rat hippocampal neurons.  |  Yoon, KW., et al. 1993. J Physiol. 464: 423-39. PMID: 8229811

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Picrotoxin, 1 g

sc-202765
1 g
$66.00

Picrotoxin, 5 g

sc-202765A
5 g
$280.00

Picrotoxin, 25 g

sc-202765B
25 g
$1300.00

At what temperature should I store 100mM picrotoxin in DMSO? How long is it stable in those storage conditions? Can it go through multiple freeze/thaw cycles if it is stored in DMSO and still remain active?

Asked by: andrewismyname
Thank you for your question. We recommend storing Picrotoxin undissolved and at room temperature and to prepare each batch fresh. We do not have stability data of this compound in DMSO.
Answered by: Tech Support Europe
Date published: 2020-06-15
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Rated 5 out of 5 by from Great productThe PTX is with consistent quality. Highly recommended.
Date published: 2021-08-03
Rated 5 out of 5 by from Consistent qualityWe have been used this chemical for 4 years and are very satisfied with its quality.
Date published: 2018-06-05
Rated 5 out of 5 by from Published paper in which we used it to elevatePublished paper in which we used it to elevate neuronal activity by treating primary mouse cortical neuron cultures.
Date published: 2015-08-12
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Picrotoxin is rated 5.0 out of 5 by 3.
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