Phenylsilatrane
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Phenylsilatrane
Phenylsilatrane is a convulsant chemical which has been used as a rodenticide. Phenylsilatrane and some of its analogs with 4-substituents of H, CH3, Cl, Br, and CSi(CH3)3 are highly toxic to mice. They have been observed in the laboratory to inhibit the 35S-''tert''-butylbicyclophosphorothionate ( TBPS) binding site ( GABA-gated chloride channel) of mouse brain membranes. See also * Atrane Atranes are a class of tricyclic molecules with three five-membered rings. It is a heterocyclic structure similar to the propellanes. It has a transannular dative bond from a nitrogen at one bridgehead to a Lewis acidic atom such as silicon or bor ... * GABAA receptor negative allosteric modulator * GABAA receptor § Ligands * Chlorophenylsilatrane References Convulsants Nitrogen heterocycles Organosilicon compounds Oxygen heterocycles Rodenticides Silicon heterocycles GABAA receptor negative allosteric modulators Phenyl compounds Atranes {{heterocyclic-stub ...
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Convulsant
A convulsant is a drug which induces convulsions and/or epileptic seizures, the opposite of an anticonvulsant. These drugs generally act as stimulants at low doses, but are not used for this purpose due to the risk of convulsions and consequent excitotoxicity. Most convulsants are antagonists (or inverse agonists) at either the GABAA or glycine receptors, or ionotropic glutamate receptor agonists. Many other drugs may cause convulsions as a side effect at high doses (e.g. bupropion, tramadol, pethidine, dextropropoxyphene, clomipramine) but only drugs whose primary action is to cause convulsions are known as convulsants. Nerve agents such as sarin, which were developed as chemical weapons, produce convulsions as a major part of their toxidrome, but also produce a number of other effects in the body and are usually classified separately. Dieldrin which was developed as an insecticide blocks chloride influx into the neurons causing hyperexcitability of the CNS and convulsions. The I ...
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Convulsants
A convulsant is a drug which induces convulsions and/or epileptic seizures, the opposite of an anticonvulsant. These drugs generally act as stimulants at low doses, but are not used for this purpose due to the risk of convulsions and consequent excitotoxicity. Most convulsants are antagonists (or inverse agonists) at either the GABAA or glycine receptors, or ionotropic glutamate receptor agonists. Many other drugs may cause convulsions as a side effect at high doses (e.g. bupropion, tramadol, pethidine, dextropropoxyphene, clomipramine) but only drugs whose primary action is to cause convulsions are known as convulsants. Nerve agents such as sarin, which were developed as chemical weapons, produce convulsions as a major part of their toxidrome, but also produce a number of other effects in the body and are usually classified separately. Dieldrin which was developed as an insecticide blocks chloride influx into the neurons causing hyperexcitability of the CNS and convulsions. The I ...
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Chlorophenylsilatrane
1-(4-Chlorophenyl)silatrane is an extremely toxic organosilicon compound which was developed by M&T Chemicals as a single-dose rodenticide. It was never registered as rodenticide, except for experimental use. 1-(4-Chlorophenyl)silatrane was one of the chemicals studied in the Project Coast. Toxicity 1-(4-Chlorophenyl)silatrane is a GABA receptor antagonist and it destroys nervous functions in the central nervous system of vertebrates, primarily in the brain and possibly in the brain stem. It's a rapid acting convulsant, causing convulsions within 1 minute in mice and rats. Death occurred within 5 minutes. It is therefore likely to induce poison shyness. In field trials, it was less effective than zinc phosphide against wild rats. See also *Phenylsilatrane Phenylsilatrane is a convulsant chemical which has been used as a rodenticide. Phenylsilatrane and some of its analogs with 4-substituents of H, CH3, Cl, Br, and CSi(CH3)3 are highly toxic to mice. They have been observed in ...
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Chloride Channel
Chloride channels are a superfamily of poorly understood ion channels specific for chloride. These channels may conduct many different ions, but are named for chloride because its concentration ''in vivo'' is much higher than other anions. Several families of voltage-gated channels and ligand-gated channels (e.g., the CaCC families) have been characterized in humans. Voltage-gated chloride channels display a variety of important physiological and cellular roles that include regulation of pH, volume homeostasis, organic solute transport, cell migration, cell proliferation and differentiation. Based on sequence homology the chloride channels can be subdivided into a number of groups. General functions Voltage-gated chloride channels are important for setting cell resting membrane potential and maintaining proper cell volume. These channels conduct or other anions such as . The structure of these channels are not like other known channels. The chloride channel subunits contain ...
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Mouse Brain
The mouse brain refers to the brain of Mus musculus. Various brain atlases exist. For reasons of reproducibility, genetically characterized, stable strains like C57BL/6 were chosen to produce high-resolution images and databases. Well known online resources include: *Allen Brain Atlas * Mouse Brain LibraryHigh resolution mouse brain atlas*BrainMaps High-Resolution Brain Maps and Brain Atlases of ''Mus musculus'' Despite superficial differences, especially in size and weight, the mouse brain and its function can serve as a powerful animal model for study of human brain diseases or mental disorders (see e.g. Reeler, Chakragati mouse). This is because the genes responsible for building and operating both mouse and human brain are 90% identical. Transgenic mouse lines also allow neuroscientists to specifically target the labeling of certain cell types to probe the neural basis of fundamental processes. Anatomy The cerebral cortex of a mouse has around 8–14 million neurons while in ...
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Atrane
Atranes are a class of tricyclic molecules with three five-membered rings. It is a heterocyclic structure similar to the propellanes. It has a transannular dative bond from a nitrogen at one bridgehead to a Lewis acidic atom such as silicon or boron at the other bridgehead.Voronkov, Mikhail G.; Baryshok, Viktor P. "Atranes - a new generation of biologically active substances" (in Russian) Vestnik Rossiiskoi Akademii Nauk 2010, volume 80, 985-992. The name "atrane" was first proposed by . Nomenclature Various atranes are named depending on the central element, e.g. "silatrane" (E = silicon); "boratrane" (E = boron); "phosphatrane" (E = phosphorus), etc. It is also proposed that when Y = nitrogen, the prefix "aza" be inserted before ''element'' + "atrane" (azasilatrane, for example) because atranes wherein E = silicon and Y = oxygen have been referred to as just "silatranes". Structure and properties Silatranes exhibit unusual properties as well as biological activity in w ...
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GABAA Receptor Negative Allosteric Modulator
A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA). They are closely related and similar to GABAA receptor antagonists. The effects of GABAA receptor NAMs are functionally the opposite of those of GABAA receptor positive allosteric modulators (PAMs) like the benzodiazepines, barbiturates, and ethanol (alcohol). Non-selective GABAA receptor NAMs can produce a variety of effects including convulsions, neurotoxicity, and anxiety, among others. Flumazenil is a competitive antagonist of the benzodiazepine site of the GABAA receptor and hence is a GABAA receptor NAM of sorts. It is used to reverse benzodiazepine overdose. The drug can provoke seizures in those with benzodiazepine dependence. Selective NAMs (or "inverse agonists") of α5 subunit-containing GABAA receptors, such as basmisanil and α5IA, do not have ...
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GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on the postsynaptic cell is selectively permeable to chloride ions (Cl−) and, to a lesser extent, bicarbonate ions (HCO3−). Depending on the membrane potential and the ionic concentration difference, this can result in ionic fluxes across the pore. If the membrane potential is higher than the equilibrium potential (also known as the reversal potential) for chloride ions, when the receptor is activated Cl− will flow into the cell. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring at the postsynaptic cell. The reversal potential of the GABAA-mediated inhibitory postsynaptic potential (IPSP) in normal solution is −70 mV, contrasting the GABAB IPSP (-100 mV). T ...
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Rodenticide
Rodenticides are chemicals made and sold for the purpose of killing rodents. While commonly referred to as "rat poison", rodenticides are also used to kill mice, squirrels, woodchucks, chipmunks, porcupines, nutria, beavers, and voles. Despite the crucial roles that rodents play in nature, there are times when they need to be controlled. Some rodenticides are lethal after one exposure while others require more than one. Rodents are disinclined to gorge on an unknown food (perhaps reflecting an adaptation to their inability to vomit), preferring to sample, wait and observe whether it makes them or other rats sick. This phenomenon of poison shyness is the rationale for poisons that kill only after multiple doses. Besides being directly toxic to the mammals that ingest them, including dogs, cats, and humans, many rodenticides present a secondary poisoning risk to animals that hunt or scavenge the dead corpses of rats. Classes of rodenticides Anticoagulants Anticoagulant ...
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TBPS
TBPS (''tert''-butylbicyclophosphorothionate) is a bicyclic phosphate convulsant. It is an extremely potent GABA receptor antagonist. See also *IPTBO *EBOB EBOB is a GABA receptor antagonist and neurotoxin. See also * TBPS *IPTBO IPTBO (isopropylbicyclophosphate, also IPPO) is a bicyclic phosphate convulsant. It is an extremely potent GABA receptor antagonist that can cause violent convulsions ... References Bicyclic phosphates Convulsants Neurotoxins Tert-butyl compounds Organothiophosphate esters Oxygen heterocycles GABAA receptor negative allosteric modulators {{Neurotoxin-stub ...
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Nitrogen Heterocycles
Nitrogen is the chemical element with the symbol N and atomic number 7. Nitrogen is a nonmetal and the lightest member of group 15 of the periodic table, often called the pnictogens. It is a common element in the universe, estimated at seventh in total abundance in the Milky Way and the Solar System. At standard temperature and pressure, two atoms of the element bond to form N2, a colorless and odorless diatomic gas. N2 forms about 78% of Earth's atmosphere, making it the most abundant uncombined element. Nitrogen occurs in all organisms, primarily in amino acids (and thus proteins), in the nucleic acids ( DNA and RNA) and in the energy transfer molecule adenosine triphosphate. The human body contains about 3% nitrogen by mass, the fourth most abundant element in the body after oxygen, carbon, and hydrogen. The nitrogen cycle describes the movement of the element from the air, into the biosphere and organic compounds, then back into the atmosphere. Many industrially importa ...
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