Picrotoxinin
A chemical compound used as a central nervous system stimulant and convulsant
Picrotoxinin is a naturally occurring chemical compound that acts as a potent central nervous system stimulant and convulsant. It is one of the two components of picrotoxin, the other being picrotin. Picrotoxinin is derived from the seeds of the plant Anamirta cocculus, commonly known as the fishberry or Indian berry.
Chemical Structure and Properties[edit | edit source]
Picrotoxinin is a sesquiterpene lactone with a complex bicyclic structure. It is characterized by its unique arrangement of carbon atoms and the presence of a lactone ring. The molecular formula of picrotoxinin is C15H16O6, and it has a molar mass of 292.28 g/mol.
The compound is a white crystalline solid that is sparingly soluble in water but more soluble in organic solvents such as ethanol and chloroform. Its chemical structure is responsible for its biological activity, particularly its ability to interact with the GABA (gamma-aminobutyric acid) receptor complex.
Mechanism of Action[edit | edit source]
Picrotoxinin acts as a non-competitive antagonist of the GABAA receptor, which is a major inhibitory neurotransmitter receptor in the central nervous system. By binding to the chloride channel of the GABAA receptor, picrotoxinin inhibits the flow of chloride ions into neurons, thereby reducing the inhibitory effects of GABA. This leads to increased neuronal excitability and can result in convulsions.
The compound is often used in research to study the function of GABAergic neurotransmission and to model seizure activity in experimental settings.
Toxicity and Safety[edit | edit source]
Picrotoxinin is highly toxic and can cause convulsions, respiratory failure, and death if ingested in sufficient quantities. It is primarily used in laboratory research and is not used therapeutically in humans. Safety precautions must be taken when handling picrotoxinin to avoid accidental exposure.
Historical and Research Uses[edit | edit source]
Historically, picrotoxin, which contains picrotoxinin, was used as a fish poison and as a stimulant in veterinary medicine. In modern research, picrotoxinin is used to study the mechanisms of epilepsy and to test the efficacy of anticonvulsant drugs.
Also see[edit | edit source]
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