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TBPO
TBPO is an extremely toxic bicyclic phosphate convulsant and GABA receptor antagonist. It is the most toxic bicyclic phosphate known, with an of 36 μg/kg in mice. 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 in mice. IPTBO is found among a group of highly toxic bicyclic phosphates. Ge ... References Convulsants Neurotoxins Bicyclic phosphates GABAA receptor negative allosteric modulators Tert-butyl compounds {{Neurotoxin-stub ...
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Bicyclic Phosphate
Bicyclic phosphate is a class of organophosphate compounds that are used as flame retardants, stabilizers and antioxidants. They are also used in spectroscopic studies. Some bicyclic phosphates, such as TBPS, TBPO and IPTBO, are highly toxic. They have toxicity comparable to nerve agents. However, they are not acetylcholinesterase inhibitors. They act as GABA receptor antagonists and have potent convulsant effects. See also *Convulsant * TBPS * 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. Ge ... References Convulsants Neurotoxins GABAA receptor negative allosteric modulators Organophosphates Phosphate esters {{Neurotoxin-stub ...
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Bicyclic Phosphates
Bicyclic phosphate is a class of organophosphate compounds that are used as flame retardants, stabilizers and antioxidants. They are also used in spectroscopic studies. Some bicyclic phosphates, such as TBPS, TBPO and IPTBO, are highly toxic. They have toxicity comparable to nerve agents. However, they are not acetylcholinesterase inhibitors. They act as GABA receptor antagonists and have potent convulsant effects. See also *Convulsant * TBPS * 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. Ge ... References Convulsants Neurotoxins GABAA receptor negative allosteric modulators Organophosphates Phosphate esters {{Neurotoxin-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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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. Generally, bicyclic phosphates disrupt chloride ion flow through GABA receptors, causing CNS overstimulation and lethal convulsions within minutes. IPTBO has these effects when injected, inhaled, or ingested and is one of the more toxic types of this antagonist. Discovery Derivatives of IPTBO are used in spectroscopic studies and as flame retardants, vinyl resin stabilizers, and antioxidants (due to their ability to terminate oxidation reactions). It had also previously been used as plane engine lubricant, and contributed to "aerotoxic syndrome". Generally speaking, toxic phosphorus esters are used as insecticides or chemical weapons (such as DFP), but unlike most phosphorus esters, IPTBO doesn’t inhibit acetylcholinesterase, despit ...
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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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GABA Receptor Antagonist
GABA receptor antagonists are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant effects, and are mainly used for counteracting overdoses of sedative drugs. Examples include bicuculline, securinine and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil. Other agents which may have GABAA receptor antagonism include the antibioticiprofloxacin tranexamic acid, thujone, ginkgo biloba, and kudzu Kudzu (; also called Japanese arrowroot or Chinese arrowroot) is a group of climbing, coiling, and trailing deciduous perennial vines native to much of East Asia, Southeast Asia, and some Pacific islands, but invasive species, invasive in many .... See also * GABAA receptor negative allosteric modulators External links * References Biochemistry {{nervous-system-drug-stub ...
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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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Neurotoxins
Neurotoxins are toxins that are destructive to nerve tissue (causing neurotoxicity). Neurotoxins are an extensive class of exogenous chemical neurological insultsSpencer 2000 that can adversely affect function in both developing and mature nervous tissue.Olney 2002 The term can also be used to classify endogenous compounds, which, when abnormally contacted, can prove neurologically toxic. Though neurotoxins are often neurologically destructive, their ability to specifically target neural components is important in the study of nervous systems. Common examples of neurotoxins include lead, ethanol (drinking alcohol), glutamate,Choi 1987 nitric oxide, botulinum toxin (e.g. Botox), tetanus toxin,Simpson 1986 and tetrodotoxin. Some substances such as nitric oxide and glutamate are in fact essential for proper function of the body and only exert neurotoxic effects at excessive concentrations. Neurotoxins inhibit neuron control over ion concentrations across the cell membrane, or c ...
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GABAA Receptor Negative Allosteric Modulators
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). Th ...
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