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Picrotoxin is an equimolar mixture of two compounds, picrotoxinin (C 15 H 16 O 6; CAS# 17617-45-7) and picrotin (C 15 H 18 O 7; CAS# 21416-53-5). [3] Of the two compounds, picrotin is less active. [4] Picrotoxin occurs naturally in the fruit of the Anamirta cocculus, a climbing plant from India and other parts of Southeast Asia. The plant is ...
Its fruit is the source of picrotoxin, a poisonous compound with stimulant properties. The plant is large-stemmed (up to 10 cm in diameter); the bark is "corky gray" with white wood. The "small, yellowish-white, sweet-scented" flowers vary between 6 and 10 millimeters across; the fruit produced is a drupe, "about 1 cm in diameter when dry". [2]
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Some naturally occurring GABA A receptor NAMs like cicutoxin and picrotoxin are considered to be toxins. Other GABA A receptor NAMs like dieldrin and fipronil are used as insecticides (IRAC group 2), and TETS is used as a rodenticide, and yet other GABA A receptor NAMs like bemegride, flurothyl, and pentylenetetrazol are used for clinical purposes.
They found that in vivo convulsant potency was strongly correlated to in vitro affinity to the picrotoxin binding site on the GABA-A receptor complex. Many GABA-A ligands, such as the sedatives diazepam and phenobarbital , are effective anticonvulsants , but presumably pentylenetetrazol has the opposite effect when it binds to the GABA-A receptor.
Chondrodendron tomentosum, the main source of 'tube curare' and principal source of D-tubocurarine (DTC), the alkaloid constituting medicinal curare Strychnos toxifera, the Strychnos species which is the principal source of 'calabash curare' and its main active constituent, the alkaloid toxiferine
Lindane is a neurotoxin that interferes with GABA neurotransmitter function by interacting with the GABA A receptor-chloride channel complex at the picrotoxin binding site. In humans, lindane affects the nervous system, liver, and kidneys, and may well be a carcinogen. [6] [7] Whether lindane is an endocrine disruptor is unclear. [8] [9] [10]