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Catalog No.
GABAA receptor antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
Ship with 10-15 days

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Picrotoxin is a noncompetitive antagonist of γ-aminobutyric acid-A (GABAA) and GABAC receptors, with IC50 value of 0.6 μM for GABAC receptors [1, 2]. 

Three classes of GABA receptors have been characterized based on their pharmacology, namely GABAA, GABAB and GABAC receptors, among which GABAA and GABAC receptors are ligand-gated chloride (Cl-) channels. GABA receptors play important roles in central nervous system by responding to the inhibitory neurotransmitter GABA [2]. 

In hippocampal cultured neurons, picrotoxin blocked GABAA-mediated currents, with an IC50 of 14 μM. Bath application of picrotoxin at 7 μM induced epileptiform activity, by blocking 30% of the GABAA-mediated receptor responses [1]. 

In male rats, i.p. injection (3 mg/kg) of picrotoxin significantly increased somatostatin (SRIF) release from the median eminence (ME) compared to baseline levels measured in the same animals, whilst local perfusion of picrotoxin did not affect SRIF release from the ME, which suggested a physiological endogenous inhibitory tone of GABA on SRIF release [3]. 


[1]. Gibbs III J W, Sombati S, DeLorenzo R J, et al. Physiological and pharmacological alterations in postsynaptic GABA(A) receptor function in a hippocampal culture model of chronic spontaneous seizures. Journal of Neurophysiology, 1997, 77(4): 2139-2152.

[2]. Goutman J D, Calvo D J. Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptor. British Journal of Pharmacology, 2004, 141(4): 717-727.

[3]. Arancibia S, Briozzo P. Peripheral administration of picrotoxin and bicuculline stimulates in vivo somatostatin release from rat median eminence. Neuroscience Letters, 1990, 111(1-2): 211-216.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.124-87-8
Solubility≥24.55 mg/mL in DMSO; ≥2.3 mg/mL in H2O with gentle warming and ultrasonic; ≥45.2 mg/mL in EtOH
SDFDownload SDF
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure