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Miotine
Miotine is an acetylcholinesterase inhibitor, anticholinesterase drug. Miotine was the first synthetic carbamate that was used clinically. Unlike the miotine analog neostigmine, it doesn't have a quaternary ammonium group to give it a permanent positive charge. It can exist as an uncharged Freebase (chemistry), free base which could allow it to cross the blood–brain barrier and cause unwanted central nervous system (CNS) side effects. : See also *Neostigmine *T-1123 *TL-1238 *TMTFA References [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
T-1123
T-1123 is a carbamate-based acetylcholinesterase inhibitor. It was investigated as a chemical warfare agent starting in 1940. It does not go through the blood-brain barrier due to the charge on quaternary nitrogen. The antidote is atropine. T-1123 is a quaternary ammonium ion. A phenyl carbamate ester is bonded in the meta position to the nitrogen on a diethylmethyl amine. The chloride and methylsulfate salt of T-1123 is TL-1299 and TL-1317, respectively. Synthesis T-1123 can be produced from m-diethylaminophenol, methyl isocyanate and methyl iodide Iodomethane, also called methyl iodide, and commonly abbreviated "MeI", is the chemical compound with the formula CH3I. It is a dense, colorless, volatile liquid. In terms of chemical structure, it is related to methane by replacement of one h .... First, m-diethylaminophenol is reacted with methyl isocyanate to produce a methylcarbamate. The resulting methylcarbamate is then reacted with methyl iodide to produce T-1123. See ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TL-1238
TL-1238 (Substance 3393) is an extremely potent carbamate acetylcholinesterase inhibitor. It has been shown to be more potent than the parent compound neostigmine. See also * Miotine *Neostigmine * T-1123 *T-1152 *T-1194 *TL-599 TL-599, also known as SB-8, is an extremely potent carbamate class acetylcholinesterase inhibitor. See also *Neostigmine * Miotine * T-1123 * T-1152 * T-1194 * TL-1238 *Physostigmine Physostigmine (also known as eserine from ''éséré'', th ... References Acetylcholinesterase inhibitors Aromatic carbamates Quaternary ammonium compounds Phenol esters Carbamate nerve agents {{Ester-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetylcholinesterase Inhibitor
Acetylcholinesterase inhibitors (AChEIs) also often called cholinesterase inhibitors, inhibit the enzyme acetylcholinesterase from breaking down the neurotransmitter acetylcholine into choline and acetate, thereby increasing both the level and duration of action of acetylcholine in the central nervous system, autonomic ganglia and neuromuscular junctions, which are rich in acetylcholine receptors. Acetylcholinesterase inhibitors are one of two types of cholinesterase inhibitors; the other being butyryl-cholinesterase inhibitors. Acetylcholinesterase is the primary member of the cholinesterase enzyme family. Acetylcholinesterase inhibitors are classified as reversible, irreversible, or quasi-irreversible (also called pseudo-irreversible). Mechanism of action Organophosphates Organophosphates like tetraethyl pyrophosphate (TEPP) and sarin inhibit cholinesterases, enzymes that hydrolyze the neurotransmitter acetylcholine. The active centre of cholinesterases feature ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carbamate
In organic chemistry, a carbamate is a category of organic compounds with the general Chemical formula, formula and Chemical structure, structure , which are formally Derivative (chemistry), derived from carbamic acid (). The term includes organic compounds (e.g., the ester ethyl carbamate), formally obtained by replacing one or more of the hydrogen atoms by other organic functional groups; as well as salt (chemistry), salts with the carbamate anion (e.g. ammonium carbamate). Polymers whose repeat units are joined by carbamate like groups are an important family of plastics, the polyurethanes. See for clarification. Properties While carbamic acids are unstable, many carbamate esters and salt (chemistry), salts are stable and well known. Equilibrium with carbonate and bicarbonate In water solutions, the carbamate anion slowly equilibrates with the ammonium cation and the carbonate or bicarbonate anions: : : Calcium carbamate is soluble in water, whereas calcium carbona ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neostigmine
Neostigmine, sold under the brand name Bloxiverz, among others, is a medication used to treat myasthenia gravis, Ogilvie syndrome, and urinary retention without the presence of a blockage. It is also used in anaesthesia to end the effects of non-depolarising neuromuscular blocking medication. It is given by injection either into a vein, muscle, or under the skin. After injection effects are generally greatest within 30 minutes and last up to 4 hours. Common side effects include nausea, increased saliva, crampy abdominal pain, and slow heart rate. More severe side effects include low blood pressure, weakness, and allergic reactions. It is unclear if use in pregnancy is safe for the baby. Neostigmine is in the cholinergic family of medications. It works by blocking the action of acetylcholinesterase and therefore increases the levels of acetylcholine. Neostigmine was patented in 1931. It is on the World Health Organization's List of Essential Medicines. The term is from G ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ammonium Group
Ammonium is a modified form of ammonia that has an extra hydrogen atom. It is a positively charged (cationic) molecular ion with the chemical formula or . It is formed by the addition of a proton (a hydrogen nucleus) to ammonia (). Ammonium is also a general name for positively charged (protonated) substituted amines and quaternary ammonium cations (), where one or more hydrogen atoms are replaced by organic or other groups (indicated by R). Not only is ammonium a source of nitrogen and a key metabolite for many living organisms, but it is an integral part of the global nitrogen cycle. As such, human impact in recent years could have an effect on the biological communities that depend on it. Acid–base properties The ammonium ion is generated when ammonia, a weak base, reacts with Brønsted acids (proton donors): : The ammonium ion is mildly acidic, reacting with Brønsted bases to return to the uncharged ammonia molecule: : Thus, the treatment of concentrated solutio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Freebase (chemistry)
In chemistry, a free base (freebase, free-base) is a term for the neutral form of an amine or other Lewis base. The term is used in the pharmaceutical industry in contrast to salt-based formulations like hydrochlorides. The amine is often an alkaloid, such as nicotine, cocaine, morphine, and ephedrine, or derivatives thereof. Colloquially, "free-basing" also means the treatment of salts or other formulations to convert them into the free base form, especially for recreational drugs. Properties Some alkaloids are more stable as ionic salts than as free base. The salts usually exhibit greater water solubility. Common counterions include chloride, bromide, sulfate, phosphate, nitrate, acetate, oxalate, citrate, and tartrate. Amine salts formed from the acid–base reaction with hydrochloric acid are known as hydrochlorides. For example, compare the free base hydroxylamine (NH2OH) with the salt hydroxylamine hydrochloride (NH3OH+ Cl−). Freebasing Cocaine hydrochlori ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Blood–brain Barrier
The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that regulates the transfer of solutes and chemicals between the circulatory system and the central nervous system, thus protecting the brain from harmful or unwanted substances in the blood. The blood–brain barrier is formed by endothelial cells of the Capillary, capillary wall, astrocyte end-feet ensheathing the capillary, and pericytes embedded in the capillary basement membrane. This system allows the passage of some small molecules by passive transport, passive diffusion, as well as the selective and active transport of various nutrients, ions, organic anions, and macromolecules such as glucose and amino acids that are crucial to neural function. The blood–brain barrier restricts the passage of pathogens, the diffusion of solutes in the blood, and Molecular mass, large or Hydrophile, hydrophilic molecules into the cerebrospinal fluid, while a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Central Nervous System
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain, spinal cord and retina. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all parts of the bodies of bilateria, bilaterally symmetric and triploblastic animals—that is, all multicellular animals except sponges and Coelenterata, diploblasts. It is a structure composed of nervous tissue positioned along the Anatomical_terms_of_location#Rostral,_cranial,_and_caudal, rostral (nose end) to caudal (tail end) axis of the body and may have an enlarged section at the rostral end which is a brain. Only arthropods, cephalopods and vertebrates have a true brain, though precursor structures exist in onychophorans, gastropods and lancelets. The rest of this article exclusively discusses the vertebrate central nervous system, which is radically distinct from all other animals. Overview In vertebrates, the brain and spinal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neostigmine
Neostigmine, sold under the brand name Bloxiverz, among others, is a medication used to treat myasthenia gravis, Ogilvie syndrome, and urinary retention without the presence of a blockage. It is also used in anaesthesia to end the effects of non-depolarising neuromuscular blocking medication. It is given by injection either into a vein, muscle, or under the skin. After injection effects are generally greatest within 30 minutes and last up to 4 hours. Common side effects include nausea, increased saliva, crampy abdominal pain, and slow heart rate. More severe side effects include low blood pressure, weakness, and allergic reactions. It is unclear if use in pregnancy is safe for the baby. Neostigmine is in the cholinergic family of medications. It works by blocking the action of acetylcholinesterase and therefore increases the levels of acetylcholine. Neostigmine was patented in 1931. It is on the World Health Organization's List of Essential Medicines. The term is from G ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TMTFA
TMTFA is an extremely potent acetylcholinesterase inhibitor. As a transition state analog of acetylcholinesterase, TMTFA is able to inhibit acetylcholinesterase at extremely low concentrations (within the femtomolar range), making it one of the most potent acetylcholinesterase inhibitors known. Mechanism of action TMTFA has a reactive ketone group that can covalently bind to the serine residue in the active site of acetylcholinesterase. This is due to the electron-withdrawing trifluoromethyl group on the carbonyl group. See also *Acetylcholinesterase inhibitor * Methylfluorophosphonylcholine *Transition state analog Transition state analogs (transition state analogues), are chemical compounds with a chemical structure that resembles the transition state of a substrate molecule in an enzyme-catalyzed chemical reaction. Enzymes interact with a substrate by mea ... References {{Acetylcholine metabolism and transport modulators Acetylcholinesterase inhibitors Quaternary amm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
