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Picrotoxin
Picrotoxin, also known as cocculin, is a poisonous crystalline plant compound. It was first isolated by the French pharmacist and chemist Pierre François Guillaume Boullay (1777–1869) in 1812. The name "picrotoxin" is a combination of the Greek words "picros" (bitter) and "toxicon" (poison). A mixture of two different compounds, picrotoxin occurs naturally in the fruit of the '' Anamirta cocculus'' plant, although it can also be synthesized chemically. Due to its interactions with the inhibitory neurotransmitter GABA, picrotoxin acts as a stimulant and convulsant. It mainly impacts the central nervous system, causing seizures and respiratory paralysis in high enough doses. Chemical structure and synthesis Picrotoxin is an equi molar mixture of two compounds, picrotoxinin (C15H16O6; CAS# 17617-45-7) and picrotin (C15H18O7; CAS# 21416-53-5). Of the two compounds, picrotin is less active. Picrotoxin occurs naturally in the fruit of the ''Anamirta cocculus'', a climbing plant f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Picrotin Synthesis
Picrotoxin, also known as cocculin, is a poisonous crystalline plant compound. It was first isolated by the French pharmacist and chemist Pierre François Guillaume Boullay (1777–1869) in 1812. The name "picrotoxin" is a combination of the Greek words "picros" (bitter) and "toxicon" (poison). A mixture of two different compounds, picrotoxin occurs naturally in the fruit of the ''Anamirta cocculus'' plant, although it can also be synthesized chemically. Due to its interactions with the inhibitory neurotransmitter GABA, picrotoxin acts as a stimulant and convulsant. It mainly impacts the central nervous system, causing seizures and respiratory paralysis in high enough doses. Chemical structure and synthesis Picrotoxin is an equi molar mixture of two compounds, picrotoxinin (C15H16O6; CAS# 17617-45-7) and picrotin (C15H18O7; CAS# 21416-53-5). Of the two compounds, picrotin is less active. Picrotoxin occurs naturally in the fruit of the ''Anamirta cocculus'', a climbing plant fr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Picrotoxinin Synthesis
Picrotoxin, also known as cocculin, is a poisonous crystalline plant compound. It was first isolated by the French pharmacist and chemist Pierre François Guillaume Boullay (1777–1869) in 1812. The name "picrotoxin" is a combination of the Greek words "picros" (bitter) and "toxicon" (poison). A mixture of two different compounds, picrotoxin occurs naturally in the fruit of the ''Anamirta cocculus'' plant, although it can also be synthesized chemically. Due to its interactions with the inhibitory neurotransmitter GABA, picrotoxin acts as a stimulant and convulsant. It mainly impacts the central nervous system, causing seizures and respiratory paralysis in high enough doses. Chemical structure and synthesis Picrotoxin is an equi molar mixture of two compounds, picrotoxinin (C15H16O6; CAS# 17617-45-7) and picrotin (C15H18O7; CAS# 21416-53-5). Of the two compounds, picrotin is less active. Picrotoxin occurs naturally in the fruit of the ''Anamirta cocculus'', a climbing plant fr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 convu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anamirta Cocculus
''Anamirta cocculus'' ( mr, काकमारी) is a Southeast Asian and Indian climbing plant. Its fruit is the source of picrotoxin, a poisonous compound with stimulant properties. The plant is large-stemmed (up to 10 cm in diameter); the bark is "corky gray" with white wood. The "small, yellowish-white, sweet-scented" flowers vary between 6 and 10 millimeters across; the fruit produced is a drupe, "about 1 cm in diameter when dry". Chemical substances The stem and the roots contain quaternary alkaloids, such as berberine, palmatine, magnoflorine and columbamine. The seeds deliver picrotoxin, a sesquiterpene, while the seed shells contain the tertiary alkaloids menispermine and paramenispermine. Uses Its crushed seeds are an effective pediculicide (anti-lice) and are also traditionally used to stun fish or as a pesticide. In pharmacology, it is known as Cocculus Indicus. Although poisonous, hard multum is a preparation made from ''Cocculus Indicus'', et ... [...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. 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 no ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloride Channel Blockers
The chloride ion is the anion (negatively charged ion) Cl−. It is formed when the element chlorine (a halogen) gains an electron or when a compound such as hydrogen chloride is dissolved in water or other polar solvents. Chloride salts such as sodium chloride are often very soluble in water.Green, John, and Sadru Damji. "Chapter 3." ''Chemistry''. Camberwell, Vic.: IBID, 2001. Print. It is an essential electrolyte located in all body fluids responsible for maintaining acid/base balance, transmitting nerve impulses and regulating liquid flow in and out of cells. Less frequently, the word ''chloride'' may also form part of the "common" name of chemical compounds in which one or more chlorine atoms are covalently bonded. For example, methyl chloride, with the standard name chloromethane (see IUPAC books) is an organic compound with a covalent C−Cl bond in which the chlorine is not an anion. Electronic properties A chloride ion (diameter 167 pm) is much larger t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epoxides
In organic chemistry, an epoxide is a cyclic ether () with a three-atom ring. This ring approximates an equilateral triangle, which makes it strained, and hence highly reactive, more so than other ethers. They are produced on a large scale for many applications. In general, low molecular weight epoxides are colourless and nonpolar, and often volatile. Nomenclature A compound containing the epoxide functional group can be called an epoxy, epoxide, oxirane, and ethoxyline. Simple epoxides are often referred to as oxides. Thus, the epoxide of ethylene (C2H4) is ethylene oxide (C2H4O). Many compounds have trivial names; for instance, ethylene oxide is called "oxirane". Some names emphasize the presence of the epoxide functional group, as in the compound ''1,2-epoxyheptane'', which can also be called ''1,2-heptene oxide''. A polymer formed from epoxide precursors is called an ''epoxy'', but such materials do not contain epoxide groups (or contain only a few residual epoxy g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactones
Lactones are cyclic carboxylic esters, containing a 1-oxacycloalkan-2-one structure (), or analogues having unsaturation or heteroatoms replacing one or more carbon atoms of the ring. Lactones are formed by intramolecular esterification of the corresponding hydroxycarboxylic acids, which takes place spontaneously when the ring that is formed is five- or six-membered. Lactones with three- or four-membered rings (α-lactones and β-lactones) are very reactive, making their isolation difficult. Special methods are normally required for the laboratory synthesis of small-ring lactones as well as those that contain rings larger than six-membered. Nomenclature Lactones are usually named according to the precursor acid molecule (''aceto'' = 2 carbon atoms, ''propio'' = 3, ''butyro'' = 4, ''valero'' = 5, ''capro'' = 6, etc.), with a ''-lactone'' suffix and a Greek letter prefix that specifies the number of carbon atoms in the heterocycle — that is, the distance between the relevant -OH ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glycine Receptor Antagonists
Glycine (symbol Gly or G; ) is an amino acid that has a single hydrogen atom as its side chain. It is the simplest stable amino acid ( carbamic acid is unstable), with the chemical formula NH2‐ CH2‐ COOH. Glycine is one of the proteinogenic amino acids. It is encoded by all the codons starting with GG (GGU, GGC, GGA, GGG). Glycine is integral to the formation of alpha-helices in secondary protein structure due to its compact form. For the same reason, it is the most abundant amino acid in collagen triple-helices. Glycine is also an inhibitory neurotransmitter – interference with its release within the spinal cord (such as during a ''Clostridium tetani'' infection) can cause spastic paralysis due to uninhibited muscle contraction. It is the only achiral proteinogenic amino acid. It can fit into hydrophilic or hydrophobic environments, due to its minimal side chain of only one hydrogen atom. History and etymology Glycine was discovered in 1820 by the French chemist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA-rho Receptor Negative Allosteric Modulators
The GABAA-rho receptor (previously known as the GABAC receptor) is a subclass of GABAA receptors composed entirely of rho (ρ) subunits. GABAA receptors including those of the ρ-subclass are ligand-gated ion channels responsible for mediating the effects of gamma-amino butyric acid ( GABA), the major inhibitory neurotransmitter in the brain. The GABAA-ρ receptor, like other GABAA receptors, is expressed in many areas of the brain, but in contrast to other GABAA receptors, the GABAA-ρ receptor has especially high expression in the retina. Nomenclature A second type of ionotropic GABA receptor, insensitive to typical allosteric modulators of GABAA receptor channels such as benzodiazepines and barbiturates, was designated GABAС receptor. Native responses of the GABAC receptor type occur in retinal bipolar or horizontal cells across vertebrate species. GABAС receptors are exclusively composed of ρ (rho) subunits that are related to GABAA receptor subunits. Although the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pediculicide
The treatment of human lice is the removal of head lice parasites from human hair. It has been debated and studied for centuries. However, the number of cases of human louse infestations (or pediculosis) has increased worldwide since the mid-1960s, reaching hundreds of millions annually. There is no product or method that assures 100% destruction of the eggs and hatched lice after a single treatment. However, there are a number of treatment modalities that can be employed with varying degrees of success. These methods include chemical treatments, natural products, combs, shaving, hot air, and silicone-based lotions. Treatment is recommended only after a clear diagnosis since all treatments have potential side effects. Louse eggs hatch 6–9 days after oviposition. Therefore, a common recommendation is to repeat treatment with a pediculicide at least once after 10 days, when all lice have hatched. Between the two treatments (Days 2–9) the person will still be infested with lice t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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