|
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 bo ... * 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convulsant
A convulsant is a drug which induces convulsions 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 poor therapeutic indices. Most convulsants are antagonists (or inverse agonists) at either the GABAA or/and glycine receptors (e.g the pesticide fipronil), or ionotropic glutamate receptor agonists (e.g the marine toxin domoic acid). 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 causin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convulsants
A convulsant is a drug which induces convulsions 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 poor therapeutic index, therapeutic indices. Most convulsants are Receptor antagonist, antagonists (or inverse agonists) at either the GABA-A receptor, GABAA or/and glycine receptors (e.g the pesticide fipronil), or Ligand-gated ion channel, ionotropic glutamate receptor agonists (e.g the marine toxin domoic acid). 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 a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 A convulsant is a drug which induces convulsions 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 poor therapeutic indices. Most 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABA
GABA (gamma-aminobutyric acid, γ-aminobutyric acid) is the chief inhibitory neurotransmitter in the developmentally mature mammalian central nervous system. Its principal role is reducing neuronal excitability throughout the nervous system. GABA is sold as a dietary supplement in many countries. It has been traditionally thought that exogenous GABA (i.e., taken as a supplement) does not cross the blood–brain barrier, but data obtained from more recent research (2010s) in rats describes the notion as being unclear. The carboxylate form of GABA is γ-aminobutyrate. Function Neurotransmitter Two general classes of GABA receptor are known: * GABAA in which the receptor is part of a ligand-gated ion channel complex * GABAB metabotropic receptors, which are G protein-coupled receptors that open or close ion channels via intermediaries (G proteins) Neurons that produce GABA as their output are called GABAergic neurons, and have chiefly inhibitory action at receptors in t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ion channel, voltage-gated channels and ligand-gated ion channel, ligand-gated channels (e.g., the CaCC families) have been characterized in humans. Voltage-gated chloride channels perform numerous crucial physiological and cellular functions, such as controlling pH, volume homeostasis, transporting organic solutes, regulating cell migration, 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 k ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mouse Brain
A mouse (: mice) is a small rodent. Characteristically, mice are known to have a pointed snout, small rounded ears, a body-length scaly tail, and a high breeding rate. The best known mouse species is the common house mouse (''Mus musculus''). Mice are also popular as pets. In some places, certain kinds of Apodemus, field mice are locally common. They are known to invade homes for food and shelter. Mice are typically distinguished from rats by their size. Generally, when a muroid rodent is discovered, its common name includes the term ''mouse'' if it is smaller, or ''rat'' if it is larger. The common terms ''rat'' and ''mouse'' are not Taxonomy (biology), taxonomically specific. Typical mice are classified in the genus ''Mus (genus), Mus'', but the term ''mouse'' is not confined to members of ''Mus'' and can also apply to species from other genera such as the deer mouse, deer mouse (''Peromyscus''). Fancy mouse, Domestic mice sold as pets often differ substantially in size f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 Boron is a chemical element; it has symbol B and atomic number 5. In its crystalline form it is a brittle, dark, lustrous metalloid; in its amorphous form it is a brown powder. As the lightest element of the boron group it has three ...); "phosphatrane" (E = phosphorus), etc. It is also proposed that when Y = nitrogen, the prefix "aza" be inserted be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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. Selective NAMs (or "inverse agonists") of α5 subunit-containing GABAA receptors, such as basmisanil and α5IA, do not have convulsant or anxiogenic effects but instead show cognitive- and memory-enhancing or nootropic-like effects. They are under investigation for the treatment of cognitive impairment in conditions like Down syndrome and schizophrenia. In addition, th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous Ligand (biochemistry), ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Accurate regulation of GABAergic transmission through appropriate developmental processes, specificity to neural cell types, and responsiveness to activity is crucial for the proper functioning of nearly all aspects of the central nervous system (CNS). Upon opening, the GABAA receptor on the Chemical synapse, postsynaptic cell is selectively permeable to Chloride, chloride ions () and, to a lesser extent, Bicarbonate, bicarbonate ions (). GABAAR are members of the ligand-gated ion channel receptor superfamily, which is a chloride channel family with a dozen or more heterotetrametric subtypes and 19 distinct subunits. These subtypes have distinct brain regional and subcellular localization, age-dependent expression, and the ability to undergo plastic alt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, woodchucks, chipmunks, porcupines, nutria, beavers, and voles. 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 Anticoagulants are defined as chronic (death occurs one to two weeks after ingestion of the lethal dose, rarely sooner), single-d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TBPS
TBPS (''tert''-butylbicyclophosphorothionate) is a bicyclic phosphate convulsant. It is an extremely potent GABA receptor antagonist. See also * TBPO *IPTBO IPTBO (isopropylbicyclophosphate, also IPPO) is a bicyclic phosphate convulsant. It is an extremely potent GABA receptor antagonist that can cause violent convulsions in mice. IPTBO is found among a group of highly toxic bicyclic phosphates. Gen ... * EBOB References Bicyclic phosphates Convulsants Neurotoxins Tert-butyl compounds Organothiophosphate esters Oxygen heterocycles GABAA receptor negative allosteric modulators {{Neurotoxin-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrogen Heterocycles
Nitrogen is a chemical element; it has 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 colourless and odourless diatomic gas. N2 forms about 78% of Earth's atmosphere, making it the most abundant chemical species in air. Because of the volatility of nitrogen compounds, nitrogen is relatively rare in the solid parts of the Earth. It was first discovered and isolated by Scottish physician Daniel Rutherford in 1772 and independently by Carl Wilhelm Scheele and Henry Cavendish at about the same time. The name was suggested by French chemist Jean-Antoine-Claude Chaptal in 1790 when it was found that nitrogen was present in nitric acid and nitrates. Antoine Lavoisier suggested instead the nam ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
