| Bioactivity | Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM[1]. | ||||||||||||
| Target | IC50: 1.15 μM (GABAA receptor) | ||||||||||||
| Invitro | Picrotoxinin (0.001 µM-1 mM; 60-90 s) inhibits the action of GABAA receptor and regulates GABAA modulators in the presence of EC5 GABA at α1β2γ2L GABAA receptors[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | Picrotoxinin | ||||||||||||
| CAS | 17617-45-7 | ||||||||||||
| Formula | C15H16O6 | ||||||||||||
| Molar Mass | 292.28 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ng CC, et al. Effects of bilobalide, ginkgolide B and picrotoxinin on GABAA receptor modulation by structurally diverse positive modulators. Eur J Pharmacol. 2017 Jul 5;806:83-90. |