[2] A mixture of two different compounds, picrotoxin occurs naturally in the fruit of the Anamirta cocculus plant, although it can also be synthesized chemically.

It mainly impacts the central nervous system, causing seizures and respiratory paralysis in high enough doses.

[4] Picrotoxin occurs naturally in the fruit of the Anamirta cocculus, a climbing plant from India and other parts of Southeast Asia.

[7] The June 2020 synthesis instead employed the quick formation of the polycyclic core, followed by the manipulation of oxidation states of key carbon atoms in order to produce the target molecule.

Under kinetically controlled conditions, this process generally results in exo cyclization and forms bridged ring systems like those found in picrotoxin.

Reaction with the nearby cis alcohol is the key obstruction, and can be inhibited by pretreatment (protection) with trifluoroacetic anhydride in pyridine:[9] Picrotoxin has also been used as a starting material in several synthetic processes, including the creation of dl-picrotoxadiene, which retains certain features of the picrotoxin skeleton.

A study by Newland and Cull-Candy found that, in high enough concentrations, picrotoxin reduced the amplitude of GABA currents.

According to the Register of Toxic Effects of Chemical Substances, the LDLo, or lowest reported lethal dose, is 0.357 mg/kg.

Symptoms of picrotoxin poisoning include coughing, difficulty breathing, headache, dizziness, confusion, gastro-intestinal distress, nausea or vomiting, and changes in heart rate and blood pressure.

Although especially dangerous if swallowed, systemic effects can also result from inhalation or absorption into the blood stream through lesions in the skin.