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Physostigmine
Physostigmine (also known as eserine from ''éséré'', the West African name for the Calabar bean) is a highly toxic parasympathomimetic alkaloid, specifically, a reversible cholinesterase inhibitor. It occurs naturally in the Calabar bean and the fruit of the Manchineel tree. The chemical was synthesized for the first time in 1935 by Percy Lavon Julian and Josef Pikl. It is available in the U.S. under the trade names Antilirium and Isopto Eserine, and as eserine salicylate and eserine sulfate. Today, physostigmine is most commonly used for its medicinal value. However, before its discovery by Robert Christison, Sir Robert Christison in 1846, it was much more prevalent as an ordeal poison. The positive medical applications of the drug were first suggested in the gold medal-winning final thesis of Thomas Richard Fraser at the University of Edinburgh in 1862. Medical uses Physostigmine, an acetylcholinesterase inhibitor, can be used to treat glaucoma and delayed gastric emptyin ...
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Alkaloid
Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large variety of organisms including bacteria, fungus, fungi, Medicinal plant, plants, and animals. They can be purified from crude extracts of these organisms by acid-base extraction, or solvent extractions followed by silica-gel column chromatography. Alkaloids have a wide range of pharmacology, pharmacological activities including antimalarial medication, antimalarial (e.g. quinine), asthma, antiasthma (e.g. ephedrine), chemotherapy, anticancer (e.g. omacetaxine mepesuccinate, homoharringtonine), cholinomimetic (e.g. galantamine), vasodilation, vasodilatory (e.g. vincamine), Antiarrhythmic agent, antiarrhythmic (e.g. quinidine), analgesic (e.g. morphine), antibacterial (e.g. chelerythrine), and anti-diabetic, antihyperglycemic activities (e.g. berb ...
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Percy Lavon Julian
Percy Lavon Julian (April 11, 1899 – April 19, 1975) was an American research chemist and a pioneer in the chemical synthesis of medicinal drugs from plants. Julian was the first person to synthesize the natural product physostigmine, and a pioneer in industrial large-scale chemical synthesis of the human hormones progesterone and testosterone from plant sterols such as stigmasterol and sitosterol. His work laid the foundation for the steroid drug industry's production of cortisone, other corticosteroids, and artificial hormones that led to birth control pills. Julian started his own company to synthesize steroid intermediates from wild Mexican yams. His work helped to greatly reduce the cost of steroid intermediates to large multinational pharmaceutical companies. This significantly expanded the use of several important drugs, including synthetic cortisone. Julian was one of the first African Americans to be allowed to earn a doctorate in chemistry. He was the first African ...
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Scopolamine
Scopolamine, also known as hyoscine, or Devil's Breath, is a medication used to treat motion sickness and postoperative nausea and vomiting. It is also sometimes used before surgery to decrease saliva. When used by injection, effects begin after about 20 minutes and last for up to 8 hours. It may also be used orally and as a transdermal patch since it has been long known to have transdermal bioavailability. Scopolamine is in the antimuscarinic family of drugs and works by blocking some of the effects of acetylcholine within the nervous system. Scopolamine was first written about in 1881 and started to be used for anesthesia around 1900. Scopolamine is also the main active component produced by certain plants of the nightshade family, which historically have been used as psychoactive drugs, known as '' deliriants'', due to their antimuscarinic-induced hallucinogenic effects in higher doses. In these contexts, its mind-altering effects have been utilized for recre ...
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Parasympathomimetic
A parasympathomimetic drug, sometimes called a cholinomimetic drug or cholinergic receptor stimulating agent, is a substance that stimulates the parasympathetic nervous system (PSNS). These chemicals are also called cholinergic drugs because acetylcholine (ACh) is the neurotransmitter used by the PSNS. Chemicals in this family can act either directly by stimulating the nicotinic or muscarinic receptors (thus mimicking acetylcholine), or indirectly by inhibiting cholinesterase, promoting acetylcholine release, or other mechanisms. Common uses of parasympathomimetics include glaucoma, Sjögren syndrome and underactive bladder. Some chemical weapons such as sarin or VX, non-lethal riot control agents such as tear gas, and insecticides such as diazinon fall into this category. Structure activity relationships for parasympathomimetic drugs For a cholinergic agent, the following criteria describe the structure activity relationship: # Ing's Rule of 5: there should be no ...
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Anticholinergic
Anticholinergics (anticholinergic agents) are substances that block the action of the acetylcholine (ACh) neurotransmitter at synapses in the central nervous system, central and peripheral nervous system. These agents inhibit the parasympathetic nervous system by selectively blocking the binding of ACh to its receptor in nerve cells. The nerve fibers of the parasympathetic system are responsible for the involuntary movement of Smooth muscle tissue, smooth muscles present in the gastrointestinal tract, urinary tract, lungs, sweat glands, and many other parts of the body. In broad terms, anticholinergics are divided into two categories in accordance with their specific targets in the central and peripheral nervous system and at the neuromuscular junction: antimuscarinic agents and antinicotinic agents (ganglionic blockers, neuromuscular blockers). The term "anticholinergic" is typically used to refer to antimuscarinics that competitively inhibit the binding of ACh to muscarinic a ...
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Antidote
An antidote is a substance that can counteract a form of poisoning. The term ultimately derives from the Greek term φάρμακον ἀντίδοτον ''(pharmakon antidoton)'', "(medicine) given as a remedy". An older term in English which is now rare is atterlothe, derived from " atter" ("poison" or "venom"). Antidotes for anticoagulants are sometimes referred to as reversal agents. The antidotes for some particular toxins are manufactured by injecting the toxin into an animal in small doses and extracting the resulting antibodies from the host animals' blood. This results in an antivenom that can be used to counteract venom produced by certain species of snakes, spiders, and other venomous animals. Some animal venoms, especially those produced by arthropods (such as certain spiders, scorpions, and bees) are only potentially lethal when they provoke allergic reactions and induce anaphylactic shock; as such, there is no "antidote" for these venoms; however anaphylactic shoc ...
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Diphenhydramine
Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative. Although generally considered sedating, diphenhydramine can cause paradoxical central nervous system stimulation in some individuals, particularly at higher doses. This may manifest as agitation, anxiety, or restlessness rather than sedation. It is a H1 antagonist#First-generation (non-selective, classical), first-generation H1-antihistamine and it works by blocking certain effects of histamine, which produces its antihistamine and sedative effects. Diphenhydramine is also a potent anticholinergic. It is mainly used to treat allergy, allergies, insomnia, and symptoms of the common cold. It is also less commonly used for tremors in parkinsonism, and nausea. It is taken oral administration, by mouth, injection into a vein, injected into a vein, injection into a muscle, injected into a muscle, or topical medication, applied to the skin. Maximal effect is typically around two hours af ...
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Atropa Belladonna
''Atropa bella-donna'', commonly known as deadly nightshade or belladonna, is a toxic perennial herbaceous plant in the nightshade family Solanaceae, which also includes tomatoes, potatoes and eggplant. It is native to Europe and Western Asia, including Turkey, its distribution extending from England in the west to western Ukraine and the Iranian province of Gilan in the east. It is also naturalised or introduced in some parts of Canada, North Africa and the United States. The foliage and berries are extremely toxic when ingested, containing tropane alkaloids. It can also be harmful to handle and/or touch these plants. These toxins include atropine, scopolamine, and hyoscyamine, which cause delirium and hallucinations, and are also used as pharmaceutical anticholinergics. Tropane alkaloids are of common occurrence not only in the Old World tribes Hyoscyameae (to which the genus Atropa belongs) and Mandragoreae, but also in the New World tribe Datureae—all of which bel ...
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Dimenhydrinate
Dimenhydrinate, also known as diphenhydramine/8-chlorotheophylline salt and sold under the brand names Dramamine and Gravol, among others, is an over-the-counter medication used to treat motion sickness and nausea. Dimenhydrinate is a theoclate salt composed of diphenhydramine and 8-chlorotheophylline (a theophylline relative) in a 1:1 ratio. Dimenhydrinate was introduced to the market by G.D. Searle in 1949. Medical uses Dimenhydrinate is an over-the-counter (OTC) first-generation antihistamine indicated for the prevention and relief of nausea and vomiting from a number of causes, including motion-sickness and post-operative nausea. Side effects Common side effects of dimenhydrinate may include drowsiness, dry mouth, nose, or throat, constipation, and blurred vision. Some individuals, particularly children, may experience feelings of restlessness or excitement. In certain cases, more severe symptoms may arise, such as delirium, weakness, and a tendency to be ...
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Eseroline
Eseroline is a drug which acts as an opioid agonist. It is a metabolite of the acetylcholinesterase inhibitor physostigmine but unlike physostigmine, the acetylcholinesterase inhibition produced by eseroline is weak and easily reversible, and it produces fairly potent analgesic effects mediated through the mu opioid receptor, μ-opioid Receptor (biochemistry), receptor. This mixture of activities gives eseroline an unusual pharmacological profile, although its uses are limited by side effects such as respiratory depression and neurotoxicity. Synthesis The alkylation of phenacetin (1) with dimethyl sulfate gives ''N''-methylphenetidine (2). Treatment with 2-bromopropanoyl bromide gives 2-bromo-''N''-(4-ethoxyphenyl)-''N''-methylpropanamide (3). Treatment with aluminium trichloride results in 1,3-dimethyl-5-hydroxyoxindole (4). Alkylation with diethyl sulfate gives 5-ethoxy-1,3-dimethylindolin-2-one (5). Base-catalyzed treatment with chloroacetonitrile gives 2-(5-ethoxy-1,3-dimethy ...
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Alzheimer's Disease
Alzheimer's disease (AD) is a neurodegenerative disease and the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in remembering recent events. As the disease advances, symptoms can include problems with language, disorientation (including easily getting lost), mood swings, loss of motivation, self-neglect, and behavioral issues. As a person's condition declines, they often withdraw from family and society. Gradually, bodily functions are lost, ultimately leading to death. Although the speed of progression can vary, the average life expectancy following diagnosis is three to twelve years. The causes of Alzheimer's disease remain poorly understood. There are many environmental and genetic risk factors associated with its development. The strongest genetic risk factor is from an allele of apolipoprotein E. Other risk factors include a history of head injury, clinical depression, and high blood pressure. The progression of the di ...
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