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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 ...
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.
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]
Binding of a ligand to a binding site on protein often triggers a change in conformation in the protein and results in altered cellular function. Hence binding site on protein are critical parts of signal transduction pathways. [10] Types of ligands include neurotransmitters, toxins, neuropeptides, and steroid hormones. [11]
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The ionotropic GABA A receptor protein complex is also the molecular target of the benzodiazepine class of tranquilizer drugs. Benzodiazepines do not bind to the same receptor site on the protein complex as does the endogenous ligand GABA (whose binding site is located between α- and β-subunits), but bind to distinct benzodiazepine binding sites situated at the interface between the α- and ...