Chemical Warfare Agents
Genetic analysis of collagen Q: roles in acetylcholinesterase and butyrylcholinesterase assembly and in synaptic structure and function. (1/406)Acetylcholinesterase (AChE) occurs in both asymmetric forms, covalently associated with a collagenous subunit called Q (ColQ), and globular forms that may be either soluble or membrane associated. At the skeletal neuromuscular junction, asymmetric AChE is anchored to the basal lamina of the synaptic cleft, where it hydrolyzes acetylcholine to terminate synaptic transmission. AChE has also been hypothesized to play developmental roles in the nervous system, and ColQ is also expressed in some AChE-poor tissues. To seek roles of ColQ and AChE at synapses and elsewhere, we generated ColQ-deficient mutant mice. ColQ-/- mice completely lacked asymmetric AChE in skeletal and cardiac muscles and brain; they also lacked asymmetric forms of the AChE homologue, butyrylcholinesterase. Thus, products of the ColQ gene are required for assembly of all detectable asymmetric AChE and butyrylcholinesterase. Surprisingly, globular AChE tetramers were also absent from neonatal ColQ-/- muscles, suggesting a role for the ColQ gene in assembly or stabilization of AChE forms that do not themselves contain a collagenous subunit. Histochemical, immunohistochemical, toxicological, and electrophysiological assays all indicated absence of AChE at ColQ-/- neuromuscular junctions. Nonetheless, neuromuscular function was initially robust, demonstrating that AChE and ColQ do not play obligatory roles in early phases of synaptogenesis. Moreover, because acute inhibition of synaptic AChE is fatal to normal animals, there must be compensatory mechanisms in the mutant that allow the synapse to function in the chronic absence of AChE. One structural mechanism appears to be a partial ensheathment of nerve terminals by Schwann cells. Compensation was incomplete, however, as animals lacking ColQ and synaptic AChE failed to thrive and most died before they reached maturity. (+info)
The anticancer prodrug CPT-11 is a potent inhibitor of acetylcholinesterase but is rapidly catalyzed to SN-38 by butyrylcholinesterase. (2/406)Patients treated with high doses of CPT-11 rapidly develop a cholinergic syndrome that can be alleviated by atropine. Although CPT-11 was not a substrate for acetylcholinesterase (AcChE), in vitro assays confirmed that CPT-11 inhibited both human and electric eel AcChE with apparent K(i)s of 415 and 194 nM, respectively. In contrast, human or equine butyryl-cholinesterase (BuChE) converted CPT-11 to SN-38 with K(m)s of 42.4 and 44.2 microM for the human and horse BuChE, respectively. Modeling of CPT-11 within the predicted active site of AcChE and BuChE corroborated experimental results indicating that, although the drug was oriented correctly for activation, the constraints dictated by the active site gorge were such that CPT-11 would be unlikely to be activated by AcChE. (+info)
Cholinesterases in neural development: new findings and toxicologic implications. (3/406)Developing animals are more sensitive than adults to acute cholinergic toxicity from anticholinesterases, including organophosphorus pesticides, when administered in a laboratory setting. It is also possible that these agents adversely affect the process of neural development itself, leading to permanent deficits in the architecture of the central and peripheral nervous systems. Recent observations indicate that organophosphorus exposure can affect DNA synthesis and cell survival in neonatal rat brain. New evidence that acetylcholinesterase may have a direct role in neuronal differentiation provides additional grounds for interest in the developmental toxicity of anticholinesterases. For example, correlative anatomic studies show that transient bursts of acetylcholinesterase expression often coincide with periods of axonal outgrowth in maturing avian, rodent, and primate brain. Some selective cholinesterase inhibitors effectively suppress neurite outgrowth in model systems like differentiating neuroblastoma cells and explanted sensory ganglia. When enzyme expression is altered by genetic engineering, acetylcholinesterase levels on the outer surface of transfected neurons correlate with ability to extend neurites. Certain of these "morphogenic" effects may depend on protein-protein interactions rather than catalytic acetylcholinesterase activity. Nonetheless, it remains possible that some pesticides interfere with important developmental functions of the cholinesterase enzyme family. (+info)
Failure to confirm a synergistic effect between the K-variant of the butyrylcholinesterase gene and the epsilon4 allele of the apolipoprotein gene in Japanese patients with Alzheimer's disease. (4/406)To confirm a synergistic effect between the polymorphic K variant of the butyrylcholinesterase (BChE-K) gene and the epsilon4 allele of the apolipoprotein E (APOE) gene in Alzheimer's disease, the frequency of the BChE-K allele was re-examined in a large series of Japanese patients with Alzheimer's disease and controls. Two hundred and three patients with Alzheimer's disease and 288 age and sex matched controls were genotyped by polymerase chain reaction and restriction fragment length polymorphism for BChE-K and APOE. No changes were found in the frequency of BChE-K, either in the Alzheimer's disease group as a whole (0.17 v 0.14; p=0.36) or in early (0.16 v 0.16; p=0.98) or late (0.17 v 0.13; p=0.24) onset patients compared with age matched controls. The study failed to confirm the findings of a previous study which found a significantly higher incidence of BChE-K in patients with Alzheimer's disease with APOE epsilon4 allele than in controls. In the Japanese population studied here, there was no association between BChE-K and Alzheimer's disease, nor an interaction between BChE-K and APOE epsilon4 allele. (+info)
Anticholinesterase effects of huperzine A, E2020, and tacrine in rats. (5/406)AIM: To compare the anticholinesterase effects of huperzine A (Hup A), E2020, and tacrine in rats. METHODS: Spectrophotometry was used to determine AChE activity in brain and BuChE activity in serum. RESULTS: Following intragastric gavage, Hup A, E2020, and tacrine all produced dose-dependent inhibitions of brain AChE. Oral Hup A exhibited a higher inhibition than E2020 and tacrine. Tacrine was more effective in inhibiting serum BuChE correlated with severe peripheral adverse effects. The BuChE activity was less affected by Hup A and E2020. After a single oral dose of Hup A, a relatively steady state of AChE inhibition produced, which was longer than that after E2020 and tacrine. No change in the cholinesterase inhibition was seen for the 3 drugs following repeated i.g. medications. CONCLUSION: Hup A i.g. exhibited a higher efficacy, a longer duration of action, and a more selective inhibition on AChE than E2020 and tacrine. (+info)
Effects of synthetic (-)-huperzine A on cholinesterase activities and mouse water maze performance. (6/406)AIM: To compare the effects of synthetic and natural (-)-huperzine A (Hup A) on cholinesterase and mouse water maze performance. METHODS: Spectrophotometry was used to determine cholinesterase activity. Mouse water maze was used to evaluate nootropic effect. RESULTS: The IC50 of synthetic Hup A for acetylcholinesterase (AChE) of rat cortex and rat erythrocyte membrane determined in vitro were 64.7 (52.6-79.5) and 53.9 (43.6-66.6) nmol.L-1, respectively, and for butyrylcholinesterase of rat serum was 53.6 (44.9-63.8) mumol.L-1. Synthetic Hup A 0.12-0.48 mg.kg-1 ig produced a dose-dependent inhibition of brain AChE in mice. Synthetic Hup A 0.05 mg.kg-1 ig attenuated scopolamine-induced impairment of spatial memory. The efficacy of synthetic Hup A was the same as natural Hup A. CONCLUSION: Synthetic Hup A yielded an in vitro and in vivo pharmacological profile of activities similar to that of natural Hup A. (+info)
Characteristics of recombinant human butyrylcholinesterase. (7/406)AIM: To study the biochemical-pharmacological properties of the recombinant human butyrylcholinesterase (rhBChE) and thereby to size up the potential possibility of using it as a detoxifying agent in succinylcholine intoxication. METHODS: CHO-dhfr cells were transfected with plasmids by electroporation. BChE activity was determined colorimetrically by 5, 5'-dithiobis-(2-nitrobenzoic acid) (DTNB) method. Antigenicity was estimated by enzyme-linked immunosorbent assay and Western blot. RESULTS: The maximal expression amounted to 25.83 ng.h-1/10(6) cells. The rhBChE was highly similar to the native human BChE (nhBChE) in terms of its catalytic property, substrate affinity, inhibitor sensitivity, reactivation, stability, and immunoreactivity with anti-nhBChE antibodies. Mice challenged with 1.5 lethal dose of succinylcholine preincubated with rhBChE survived without any symptoms of intoxication. CONCLUSION: The rhBChE and nhBChE exhibit similar biochemical-pharmacological features. It is of potential value in practical use. (+info)
Inhibitory effects of huperzine B on cholinesterase activity in mice. (8/406)AIM: To determine the anticholinesterase properties of huperzine B (Hup B) and compare with tacrine in vitro and in vivo. METHODS: Spectrophotometry was used to determine ChE activity. RESULTS: Hup B showed much more selective inhibition to acetylcholinesterase (AChE) than tacrine. The IC50 ratios of Hup B and tacrine for butyrylcholinesterase (BuChE): AChE were 65.8 and 0.54, respectively. Hup B ig exhibited higher efficacy on the inhibition of brain AChE than that of tacrine. Tacrine was more effective in the inhibition of serum BuChE in mice with severe concomitant peripheral adverse effects than Hup B. A single ig dose of Hup B produced steady state of AChE inhibition in 4 h. CONCLUSION: Hup B exhibits higher selectivity and efficacy in the inhibition of AChE, and lower toxicity in mice than tacrine. (+info)
Butyrylcholinesterase (BuChE) is an enzyme that plays a crucial role in the breakdown of acetylcholine, a neurotransmitter that is involved in many important bodily functions. BuChE is primarily found in the blood and in the liver, but it is also present in other tissues throughout the body. In the medical field, BuChE is often measured as a way to assess liver function, as the enzyme is produced by liver cells. Abnormal levels of BuChE can be an indication of liver disease or other conditions that affect liver function. BuChE is also used as a biomarker for exposure to certain toxins, such as pesticides and heavy metals. In addition, researchers are studying BuChE as a potential target for the development of new drugs for the treatment of neurological disorders, such as Alzheimer's disease.
Butyrylthiocholine is a chemical compound that is used as a cholinergic agonist in the medical field. It is a synthetic analog of acetylcholine, a neurotransmitter that plays a key role in the transmission of signals between nerve cells in the brain and throughout the body. Butyrylthiocholine is used in research to study the effects of cholinergic agonists on various physiological processes, including muscle contraction, heart rate, and breathing. It is also used in the treatment of certain medical conditions, such as myasthenia gravis, a disorder that affects the muscles' ability to relax and contract properly. In the medical field, butyrylthiocholine is typically administered intravenously or intramuscularly. It can cause side effects such as nausea, vomiting, and diarrhea, and may also cause allergic reactions in some people. As with any medication, the use of butyrylthiocholine should be closely monitored by a qualified healthcare professional.
Acetylcholinesterase (AChE) is an enzyme that is responsible for breaking down the neurotransmitter acetylcholine (ACh) in the nervous system. ACh is a chemical messenger that is used to transmit signals between nerve cells, and AChE plays a critical role in regulating the levels of ACh in the synaptic cleft, the small gap between nerve cells where signaling occurs. In the medical field, AChE is often studied in the context of diseases that affect the nervous system, such as Alzheimer's disease, myasthenia gravis, and certain types of nerve damage. In these conditions, the activity of AChE may be altered, leading to changes in the levels of ACh in the brain and other parts of the nervous system. AChE inhibitors are drugs that are used to treat certain neurological disorders by slowing down the breakdown of ACh, thereby increasing its levels in the brain. These drugs are commonly used to treat Alzheimer's disease and myasthenia gravis, among other conditions.
Cholinesterases are a group of enzymes that break down the neurotransmitter acetylcholine in the body. There are two main types of cholinesterases: acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Acetylcholinesterase is primarily found in the synaptic clefts of nerve cells, where it breaks down acetylcholine after it has transmitted a signal across the synapse. This helps to terminate the signal and prevent overstimulation of the postsynaptic neuron. Butyrylcholinesterase is found in a variety of tissues throughout the body, including the liver, kidney, and blood. It is also found in the brain, where it plays a role in the breakdown of acetylcholine and other neurotransmitters. In the medical field, cholinesterases are important because they are often used as markers of organ function and can be used to diagnose certain diseases. For example, low levels of acetylcholinesterase activity in the blood can be a sign of organ damage or dysfunction, while high levels of butyrylcholinesterase activity can be a sign of liver disease. Cholinesterase inhibitors are also used as medications to treat certain neurological conditions, such as Alzheimer's disease and myasthenia gravis.
Tetraisopropylpyrophosphamide (TIP) is a medication that was previously used to treat certain types of cancer, such as Hodgkin's lymphoma and non-Hodgkin's lymphoma. It is a type of chemotherapy drug that works by interfering with the growth and division of cancer cells. However, TIP is no longer used for cancer treatment due to its toxic side effects and the availability of more effective and safer treatments. It is important to note that TIP is not a cure for cancer and should only be used under the guidance of a qualified healthcare professional.
Thiocholine is a chemical compound that is formed when choline, a neurotransmitter, is metabolized by the enzyme choline kinase. It is a precursor to the neurotransmitter acetylcholine and is involved in the regulation of muscle movement and memory. In the medical field, thiocholine is used as a diagnostic tool in the detection of certain liver and bile duct disorders, as well as in the treatment of certain types of cancer. It is also used as a contrast agent in imaging studies, such as magnetic resonance cholangiopancreatography (MRCP), to visualize the bile ducts and liver.
Sarin is a highly toxic nerve agent that is classified as a chemical weapon. It is a clear, colorless liquid that is odorless and tasteless, and it can be easily absorbed through the skin, eyes, and respiratory system. In the medical field, sarin is considered a chemical poison that can cause severe respiratory and neurological symptoms, including difficulty breathing, convulsions, and paralysis. Exposure to sarin can be fatal, and there is no known antidote for its effects. Treatment for sarin poisoning typically involves supportive care, such as oxygen therapy and respiratory support, as well as medications to manage symptoms and prevent further exposure.
Soman is a nerve agent that was first synthesized in 1944 by German chemists. It is a colorless, odorless, and tasteless liquid that is highly toxic and can be absorbed through the skin, eyes, and respiratory system. Soman is classified as a Schedule 1 controlled substance under the United States Controlled Substances Act and is illegal to possess, manufacture, or distribute without a valid prescription. In the medical field, soman is primarily used for research purposes to study the effects of nerve agents on the human body. It is also used in some military and law enforcement training exercises to simulate the effects of nerve agents and to test the effectiveness of protective gear and antidotes. However, the use of soman in these contexts is highly regulated and requires strict safety protocols to prevent accidental exposure.
Paraoxon is a chemical compound that is commonly used as an insecticide and acaricide. It is also used as a nerve agent in chemical warfare. In the medical field, paraoxon is primarily used as a treatment for organophosphate poisoning, which is caused by exposure to insecticides or nerve agents that contain organophosphates. Paraoxon works by inhibiting the enzyme acetylcholinesterase, which is responsible for breaking down the neurotransmitter acetylcholine in the nervous system. When acetylcholinesterase is inhibited, acetylcholine builds up in the nervous system, leading to overstimulation and potentially causing symptoms such as muscle twitching, difficulty breathing, and seizures. Paraoxon is typically administered as an antidote to reverse the effects of organophosphate poisoning and prevent further damage to the nervous system.
Dimethoate is an organophosphate insecticide that is commonly used in agriculture to control a wide range of pests, including aphids, mites, and thrips. It works by inhibiting the enzyme acetylcholinesterase, which is responsible for breaking down the neurotransmitter acetylcholine in the nervous system of insects. When acetylcholinesterase is inhibited, acetylcholine builds up in the insect's nervous system, leading to overstimulation and eventually death. In the medical field, dimethoate is not typically used as a treatment for humans. However, exposure to dimethoate can occur through inhalation, ingestion, or skin contact, and can cause a range of symptoms, including nausea, vomiting, diarrhea, dizziness, headache, and difficulty breathing. In severe cases, exposure to dimethoate can lead to seizures, coma, and death. Treatment for dimethoate poisoning typically involves supportive care, such as fluid replacement and respiratory support, as well as the use of antidotes to reverse the effects of the insecticide on the body.
In the medical field, organothiophosphorus compounds are a class of chemical compounds that contain a sulfur-phosphorus bond (P-S) attached to an organic group. These compounds are commonly used as pesticides, herbicides, and nerve agents. Organothiophosphorus compounds can cause a range of toxic effects on the body, including respiratory distress, nausea, vomiting, diarrhea, and seizures. In severe cases, exposure to these compounds can lead to death. In the medical setting, organothiophosphorus compounds are often encountered in cases of accidental or intentional exposure. Treatment typically involves the use of atropine, pralidoxime, and other medications to reverse the toxic effects of the compounds and support vital organ function.
Dichlorvos is an organophosphate insecticide that is commonly used to control pests such as cockroaches, ants, and flies. It works by inhibiting the enzyme acetylcholinesterase, which is responsible for breaking down the neurotransmitter acetylcholine in the nervous system. When acetylcholinesterase is inhibited, acetylcholine builds up in the nervous system, leading to overstimulation and eventually paralysis and death of the insect. In the medical field, dichlorvos is not typically used for human treatment, as it can be toxic to humans and other animals. Exposure to dichlorvos can cause symptoms such as nausea, vomiting, dizziness, and difficulty breathing. In severe cases, it can lead to seizures, coma, and death. However, dichlorvos is sometimes used as a pesticide in hospitals and other healthcare facilities to control pests that may pose a risk to patients and staff.
Organophosphate poisoning is a type of poisoning that occurs when a person is exposed to organophosphate chemicals. These chemicals are commonly used as pesticides, herbicides, and insecticides. They work by inhibiting the activity of an enzyme called acetylcholinesterase, which is responsible for breaking down a neurotransmitter called acetylcholine in the body. When acetylcholine levels become too high, it can cause overstimulation of the nervous system, leading to symptoms such as muscle twitching, difficulty breathing, and even death. Treatment for organophosphate poisoning typically involves supportive care, such as oxygen therapy and medications to counteract the effects of the poison. In severe cases, hospitalization may be necessary.
Acetylthiocholine is a chemical compound that is used as a neurotransmitter in the nervous system. It is a derivative of acetylcholine, which is a neurotransmitter that is involved in muscle movement and other functions. Acetylthiocholine is produced in the body when acetylcholine is broken down, and it is thought to play a role in the regulation of acetylcholine levels in the brain and other parts of the nervous system. In the medical field, acetylthiocholine is sometimes used as a diagnostic tool to test for certain types of neurological disorders, such as myasthenia gravis, which is a condition that affects the muscles and causes weakness and fatigue.
Organophosphorus compounds are a class of chemicals that contain a phosphorus atom bonded to one or more organic groups, such as alkyl, aryl, or alkoxy groups. These compounds are widely used in agriculture as pesticides, in the manufacturing of plastics, and as solvents. In the medical field, organophosphorus compounds are primarily used as nerve agents, which are toxic chemicals that interfere with the nervous system by inhibiting the enzyme acetylcholinesterase. This inhibition leads to an accumulation of acetylcholine, a neurotransmitter, in the synapses, causing overstimulation of the nervous system and potentially leading to death. Organophosphorus compounds are also used as medications to treat certain medical conditions, such as myasthenia gravis, a disorder that causes muscle weakness. However, they can also have toxic effects on the body, including nausea, vomiting, diarrhea, dizziness, and respiratory distress.
Isoflurophate is a chemical compound that is used as an herbicide. It is not typically used in the medical field.
Echothiophate Iodide is a chemical compound that is used as an anticholinergic medication. It works by blocking the action of acetylcholine, a neurotransmitter that is involved in muscle contraction and glandular secretion. Echothiophate Iodide is used to treat conditions such as glaucoma, irritable bowel syndrome, and excessive sweating (hyperhidrosis). It is usually administered as an eye drop or an injection. Side effects of Echothiophate Iodide may include dry mouth, blurred vision, dizziness, and difficulty urinating. It is important to follow the instructions of a healthcare professional when using this medication.
Organophosphates are a class of chemical compounds that contain a phosphorus atom bonded to an organic group. They are commonly used as pesticides, herbicides, and insecticides, as well as in industrial and military applications. In the medical field, organophosphates are often used as nerve agents, which can cause a range of symptoms including muscle weakness, difficulty breathing, and even death. They can also be used as medications to treat certain medical conditions, such as glaucoma and myasthenia gravis. However, exposure to organophosphates can be dangerous and can cause a range of adverse health effects, including respiratory problems, neurological damage, and even death.
Chlorpyrifos is an organophosphate insecticide that is commonly used in agriculture to control pests on crops. It is also used in some household and industrial products to kill insects and other pests. In the medical field, chlorpyrifos is not typically used as a treatment for any medical condition. However, exposure to chlorpyrifos can have harmful effects on human health, particularly on the nervous system. Long-term or repeated exposure to chlorpyrifos has been linked to a range of health problems, including developmental delays, learning difficulties, and neurobehavioral disorders. In some cases, exposure to chlorpyrifos can be fatal. It is important to use chlorpyrifos and other pesticides safely and according to the instructions provided by the manufacturer to minimize the risk of exposure.
Succinylcholine is a muscle relaxant medication that is commonly used during general anesthesia to facilitate tracheal intubation and to maintain muscle relaxation during surgery. It works by blocking the action of acetylcholine, a neurotransmitter that triggers muscle contractions. Succinylcholine is a depolarizing muscle relaxant, which means that it directly affects the muscle fibers themselves, rather than acting on the nervous system. It is a short-acting drug, with a duration of action of approximately 5-10 minutes, and is typically given intravenously. However, it can cause side effects such as muscle fasciculations, hyperkalemia, and postoperative myalgias.
Benzoylcholine is a chemical compound that is commonly used in the medical field as a muscle relaxant and a bronchodilator. It works by stimulating the release of acetylcholine, a neurotransmitter that triggers muscle contractions and relaxations. Benzoylcholine is often used in the treatment of muscle spasms, particularly in the muscles of the face and neck. It is also used to treat certain respiratory conditions, such as asthma and chronic obstructive pulmonary disease (COPD), by relaxing the muscles in the airways and improving airflow. Benzoylcholine is available as a prescription medication and is typically administered by injection or inhalation. It can cause side effects such as muscle twitching, sweating, and nausea, and may interact with other medications. As with any medication, it is important to use benzoylcholine only under the guidance of a healthcare professional.
Cocaine is a powerful stimulant drug that is derived from the leaves of the coca plant. It is a highly addictive substance that is illegal in many countries, including the United States. Cocaine is typically used as a recreational drug, but it can also be used for medical purposes, such as to treat certain medical conditions. In the medical field, cocaine is sometimes used as a local anesthetic to numb the skin and other tissues during surgery or other medical procedures. It is also sometimes used to treat certain medical conditions, such as glaucoma, because it can constrict blood vessels and reduce pressure in the eye. However, cocaine is also highly addictive and can cause a range of serious health problems, including heart attack, stroke, and respiratory failure. It is also associated with a high risk of addiction and can lead to a range of social and psychological problems. As a result, the use of cocaine for medical purposes is generally limited and is only done under the supervision of a qualified medical professional.
Aldicarb is a highly toxic organophosphate insecticide that is used to control a variety of pests, including termites, ants, and cockroaches. It works by inhibiting the enzyme acetylcholinesterase, which is responsible for breaking down the neurotransmitter acetylcholine in the nervous system. When acetylcholinesterase is inhibited, acetylcholine builds up in the nervous system, leading to overstimulation and eventually paralysis and death. In the medical field, aldicarb is not typically used for human treatment, as it is highly toxic and can cause serious health effects, including respiratory distress, convulsions, and death. However, aldicarb poisoning is a potential risk for people who handle or are exposed to the insecticide, and treatment typically involves supportive care, such as oxygen therapy and medications to manage symptoms. In severe cases, hospitalization and intensive care may be necessary.
In the medical field, oximes are a class of organic compounds that contain a functional group called an oxime group (-ONH). Oximes are used as antidotes for certain types of nerve agents, such as sarin and VX, which are highly toxic and can cause severe respiratory and cardiovascular problems. Oximes work by reacting with the nerve agent to form a less toxic compound that can be eliminated from the body. They are typically administered intravenously or intramuscularly, and their effectiveness depends on the type and amount of nerve agent exposure. There are several different types of oximes that have been developed for use as antidotes, including pralidoxime, obidoxime, and HI-6. These compounds have been shown to be effective in treating nerve agent poisoning in laboratory and clinical studies, although they may not be completely effective in all cases and can cause side effects such as nausea, vomiting, and allergic reactions.
Phenylcarbamates are a class of organic compounds that contain a phenyl group attached to a carbamate functional group (-COO-) which is a combination of a carbonyl group (-CO-) and an amine group (-NH2). They are commonly used as insecticides, fungicides, and herbicides. In the medical field, phenylcarbamates are used as anticholinergic drugs, which means they block the action of acetylcholine, a neurotransmitter that plays a role in muscle contraction and glandular secretion. Some examples of phenylcarbamates used in medicine include atropine, hyoscine, and scopolamine, which are used to treat conditions such as motion sickness, irritable bowel syndrome, and overactive bladder. Phenylcarbamates can also be used as local anesthetics, such as benzocaine, which is used to numb the skin and mucous membranes. However, they can also have side effects such as dry mouth, blurred vision, and dizziness, and can be toxic in high doses.
Tacrine is a medication that is used to treat mild to moderate symptoms of Alzheimer's disease. It works by inhibiting the breakdown of acetylcholine, a neurotransmitter that is important for memory and learning. Tacrine is available in tablet form and is usually taken three times a day. It can cause side effects such as nausea, vomiting, diarrhea, and stomach pain. It is important to take tacrine exactly as prescribed by a doctor, as taking too much can be dangerous.
Tritolyl phosphates are a class of industrial chemicals that are used as flame retardants, plasticizers, and stabilizers in a variety of products, including textiles, plastics, and coatings. They are composed of a tris(hydroxymethyl) phosphate molecule with a phosphorus atom at the center and three hydroxymethyl groups attached to it. In the medical field, tritolyl phosphates have been associated with a number of adverse health effects, including respiratory irritation, skin irritation, and cancer. They have been classified as potential carcinogens by the International Agency for Research on Cancer (IARC) and are regulated by various environmental and occupational health agencies around the world. In recent years, there has been growing concern about the potential health risks associated with tritolyl phosphates, particularly in relation to their use in consumer products. As a result, many companies have voluntarily phased out the use of tritolyl phosphates in their products, and some countries have banned their use altogether.
Pralidoxime compounds are a class of drugs used in the treatment of organophosphate poisoning. Organophosphate poisoning occurs when a person ingests or comes into contact with a chemical compound containing a phosphorus atom bonded to an oxygen atom, which inhibits the activity of an enzyme called acetylcholinesterase. This leads to an accumulation of acetylcholine in the body, which can cause symptoms such as muscle twitching, difficulty breathing, and even death. Pralidoxime compounds work by restoring the activity of acetylcholinesterase by chelating with the phosphorylated enzyme, allowing it to break down acetylcholine and return to its normal function. This helps to reverse the symptoms of organophosphate poisoning and prevent further damage to the body. Pralidoxime compounds are typically administered intravenously or intramuscularly, and may be given in combination with atropine, another medication used to treat organophosphate poisoning. It is important to note that pralidoxime compounds are not effective for all types of organophosphate poisoning, and their use should be determined by a healthcare professional based on the specific circumstances of the poisoning.
Diazinon is an organophosphate insecticide that has been used in agriculture and medicine to control pests and parasites. It works by inhibiting the enzyme acetylcholinesterase, which is responsible for breaking down the neurotransmitter acetylcholine in the nervous system. When acetylcholinesterase is inhibited, acetylcholine builds up in the nervous system, leading to overstimulation and potentially causing symptoms such as muscle twitching, weakness, and respiratory failure. Diazinon has been associated with a range of adverse health effects, including neurological damage, reproductive problems, and cancer. It is no longer used in the United States due to its toxicity and potential health risks.
Physostigmine is a medication that is used to treat a variety of conditions, including glaucoma, myasthenia gravis, and Alzheimer's disease. It is a natural alkaloid that is derived from the plant Physostigma venenosum, which is found in the rainforests of Southeast Asia. Physostigmine works by increasing the activity of the neurotransmitter acetylcholine in the brain and muscles, which can help to improve muscle strength and coordination, as well as improve memory and cognitive function. It is usually administered as an injection or a tablet, and it can cause side effects such as nausea, vomiting, and dizziness.
Dibenzoxazepines are a class of organic compounds that contain two benzene rings fused to an oxazepine ring. They are a subclass of the larger class of benzoxazoles, which also contain a benzene ring and an oxazole ring. Dibenzoxazepines have a variety of biological activities and are used in the treatment of a number of medical conditions, including depression, anxiety, and Parkinson's disease. They are also being studied for their potential use in the treatment of other conditions, such as Alzheimer's disease and cancer.
Undurti Narasimha Das
Raymond L. Rodriguez
RCSB PDB - 6I2T: CryoEM reconstruction of full-length, fully-glycosylated human butyrylcholinesterase tetramer
Identification of Human Butyrylcholinesterase Organophosphate-Resistant Variants through a Novel Mammalian Enzyme Functional...
Reactivation potency of two novel oximes (K456 and K733) against paraoxon-inhibited acetyl and butyrylcholinesterase: In silico...
Partial purification and characterization of soluble isoform of butyrylcholinesterase from rat intestine | AVESİS
MedlinePlus: Genes: B
An endophenotype approach to the genetics of alcohol dependence: a genome wide association study of fast beta EEG in families...
Identification of C|sub|5|/sub||sup|+|/sup| extraband of butyrylcholinesterase and two protein bands cathodic to it |...
Identification of carboxylesterase, butyrylcholinesterase, acetylcholinesterase, paraoxonase, and albumin pseudoesterase in...
Alzheimer Disease Medication: Cholinesterase Inhibitors, N-Methyl-D-Aspartate Antagonists, Combination Drugs, Monoclonal...
NIOSHTIC-2 Search Results - Full View
Sudden Infant Death Syndrome: How to protect your baby | Parenting-mums-dads - Gulf News
Department of Chemistry, Gitam Institute of Science, GITAM University, Visakhapatnam, India - Articles - Scientific Research...
Publications | Computational Biology and Drug Design Group
Identification and validation of oxidative stress and immune-related hub genes in Alzheimer's disease through bioinformatics...
Prognostic Value of Serum Cholinesterase Activity in Severe SARS-CoV-2-Infected Patients Requiring Intensive Care Unit...
Spearmint Supplement: Uses, Benefits, Side Effects, Dose
Plants | Special Issue : Antioxidant in Plants - Discovery, Biosynthesis, Regulation and Application
Wei-Jun Qian | PNNL
Seyedeh Sara MIRFAZLI | Professor (Associate) | PhD in medicinal chemistry | Iran University of Medical Sciences, Tehran |...
De novo transcriptome sequencing and digital gene expression analysis predict biosynthetic pathway of rhynchophylline and...
Biosensors for Pesticide Detection: New Trends
The Science of Gene-Environment Interaction at the Centers for Disease Control and Prevention and Agency for Toxic Substances...
<em>In Silico</em> Studies in Predicting Mechanism of Action of Amaranthus tricolor on...
Publications - Institute for Bioengineering of Catalonia
Transplantation of dorsal root ganglion into the olfactory bulb of neonatal rats: a histochemical study - IOS Press
Scientific publications : Zebrafish - Viewpoint
- The quaternary structures of the cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), are essential for their localization and function. (rcsb.org)
- Organophosphates (OPs) irreversibly inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. (simulations-plus.com)
- 4.5 × 10 -9 ), is also an expression quantitative trait locus for BCHE (butyrylcholinesterase), expressed in thalamus tissue. (nih.gov)
- Electrophoresis of human plasma yields 4 butyrylcholinesterase (BChE) protein bands, i.e. (ui.ac.id)
- A sandwich enzyme-linked immunosorbent assay (sELISA) has been developed for detection of organophosphorylated butyrylcholinesterase (OP-BChE), a potential biomarker for human exposure to organophosphate insecticides and nerve agents. (cdc.gov)
- it's regulated by the enzymes enzymes butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). (gulfnews.com)
- All compounds exhibited a good activity, and eight of them (5-8, 10, 14, 15 and 20) shared comparable low micromolar inhibitory potency versus Aβ40 aggregation and human acetylcholinesterase (AChE), while inhibiting human butyrylcholinesterase (BChE) even at submicromolar concentration. (ibecbarcelona.eu)
- Three months postoperatively the animals were perfused and their brains processed by direct thiocholine method for ch olinesterases (Ch), specific acetylcholinesterase (AChE) and nonspecific butyrylcholinesterase (BuChE) or stained by Cresyl violet. (iospress.com)
- Enzyme-linked immunosorbent assay for detection of organophosphorylated butyrylcholinesterase: a biomarker of exposure to organophosphate agents. (cdc.gov)
- Human butyrylcholinesterase (hBChE) is currently being developed as a detoxication enzyme for the catalytic hydrolysis or stoichiometric binding of organophosphates (OPs). (aspetjournals.org)
- The present group of studies first optimized the variables for extraction and solubilization of cholinesterase activity from various rat tissues and then refined an existing automated method, in order to differentially assess acetyl and butyrylcholinesterase activity in those tissues. (nih.gov)
- 8. Butyrylcholinesterase and the cholinergic system. (nih.gov)
- Human butyrylcholinesterase (hBChE) is currently being developed as a detoxication enzyme for the catalytic hydrolysis or stoichiometric binding of organophosphates (OPs). (aspetjournals.org)
- The present experiment assessed the ability of rivastigmine, a clinically utilized agent that inhibits acetylcholinesterase and butyrylcholinesterase activities, to inhibit cholinesterases in plaques and tangles. (nih.gov)
- Our Butyrylcholinesterase polyclonal, monoclonal and recombinant monoclonal antibodies are developed in Rabbit and Mouse. (thermofisher.com)
- Prolonged neuromuscular block in a patient with butyrylcholinesterase deficiency]. (nih.gov)
- The role of inheritable variations in predisposing to ADRs was shown by the correlation between drug responses and inherited deficiencies of metabolic enzymes such as pseudocholinesterase (butyrylcholinesterase) and glucose-6-phosphate dehydrogenase (G6PD).Genetic polymorphisms (variants alleles present at least in 1% of the normal population) are a source of genetic variation to drug responses. (nih.gov)
- These increases correlated with significantly inhibited fetal butyrylcholinesterase activity (Samarawickrema et al. (healthweeks.com)
- Development of a long-acting, injectable controlled release butyrylcholinesterase formulation using predictive modeling. (sbir.gov)