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Dicycloverine
Dicycloverine, also known as dicyclomine, sold under the brand name Bentyl in the US, is a medication that is used to treat spasms of the intestines such as occur in irritable bowel syndrome. It is taken by mouth or by injection into a muscle. While it has been used in baby colic and enterocolitis, evidence does not support these uses. Common side effects include dry mouth, blurry vision, weakness, sleepiness, and lightheadedness. Serious side effects may include psychosis and breathing problems in babies. Use in pregnancy appears to be safe while use during breastfeeding is not recommended. How it works is not entirely clear. Dicycloverine was approved for medical use in the United States in 1950. It is available as a generic medication. In 2020, it was the 147th most commonly prescribed medication in the United States, with more than 4million prescriptions. Medical uses Dicyclomine is used to treat the symptoms of irritable bowel syndrome, specifically hypermotility, in a ...
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Anticholinergic
Anticholinergics (anticholinergic agents) are substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the 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 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 which competitively inhibit the binding of ACh to muscarinic acetylcholine receptors; such ...
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Muscarinic Acetylcholine Receptor M4
The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the ''CHRM4'' gene. Function M4 muscarinic receptors are coupled to Gi/o heterotrimeric proteins. They function as inhibitory autoreceptors for acetylcholine. Activation of M4 receptors inhibits acetylcholine release in the striatum. The M2 subtype of acetylcholine receptor functions similarly as an inhibitory autoreceptor to acetylcholine release, albeit functioning actively primarily in the hippocampus and cerebral cortex. Muscarinic acetylcholine receptors possess a regulatory effect on dopaminergic neurotransmission. Activation of M4 receptors in the striatum inhibit D1-induced locomotor stimulation in mice. M4 receptor-deficient mice exhibit increased locomotor simulation in response to D1 agonists, amphetamine and cocaine. Neurotransmission in the striatum influences extrapyramidal motor control, thus alterations in M4 act ...
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Injection Into A Muscle
Intramuscular injection, often abbreviated IM, is the injection of a substance into a muscle. In medicine, it is one of several methods for parenteral administration of medications. Intramuscular injection may be preferred because muscles have larger and more numerous blood vessels than subcutaneous tissue, leading to faster absorption than subcutaneous or intradermal injections. Medication administered via intramuscular injection is not subject to the first-pass metabolism effect which affects oral medications. Common sites for intramuscular injections include the deltoid muscle of the upper arm and the gluteal muscle of the buttock. In infants, the vastus lateralis muscle of the thigh is commonly used. The injection site must be cleaned before administering the injection, and the injection is then administered in a fast, darting motion to decrease the discomfort to the individual. The volume to be injected in the muscle is usually limited to 2–5 milliliters, depending on inj ...
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Marion Merrell Dow
Marion Merrell Dow and its predecessor Marion Laboratories was a U.S. pharmaceutical company based in Kansas City, Missouri from 1950 until 1996. The company specialized in bringing to market drugs that had been discovered but unmarketed by other companies including Cardizem which treats arrhythmias and high blood pressure, Carafate (an ulcer treatment), Gaviscon (an antacid), Seldane (a withdrawn antihistamine), Nicorette (anti-smoking gum) and Cepacol mouthwash.Marion Merrell Dow, Inc., International Directory of Company Histories, Vol. 9. St. James Press, 1994
(reprinted on fundinguniverse.com)
The company operating out of its headquarters at 9300 Ward Parkway was a springboard for its founder ...
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Muscarinic Acetylcholine Receptor M1
The muscarinic acetylcholine receptor M1, also known as the cholinergic receptor, muscarinic 1, is a muscarinic receptor that in humans is encoded by the ''CHRM1'' gene. It is localized to 11q13. This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve, is common in exocrine glands and in the CNS. It is predominantly found bound to G proteins of class Gq that use upregulation of phospholipase C and, therefore, inositol trisphosphate and intracellular calcium as a signalling pathway. A receptor so bound would not be susceptible to CTX or PTX. However, Gi (causing a downstream decrease in cAMP) and Gs (causing an increase in cAMP) have also been shown to be involved in interactions in certain tissues, and so would be susceptible to PTX and CTX respectively. Effects * EPSP in autonomic ganglia * Secretion from salivary glands * Gastric acid secretion from stomach * In CNS (memory?) * Vagally-induced bronchoconstriction * Mediating olfac ...
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5-HT2A
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and ot ...
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Sigma-1 Receptor
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the ''SIGMAR1'' gene. The σ1 receptor is a transmembrane protein expressed in many different tissue types. It is particularly concentrated in certain regions of the central nervous system. It has been implicated in several phenomena, including cardiovascular function, schizophrenia, clinical depression, the effects of cocaine abuse, and cancer. Much is known about the binding affinity of hundreds of synthetic compounds to the σ1 receptor. An endogenous ligand for the σ1 receptor has yet to be conclusively identified, but tryptaminergic trace amines and neuroactive steroids have been found to activate the receptor. Especially progesterone, but also testosterone, pregnenolone sulfate, and dehydroepiandrosterone sulfate (DHEA-S) bind to the σ1 receptor. ...
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Endo Pharmaceuticals
Endo International plc is an American Irish-domiciled generics and specialty branded pharmaceutical company that generated over 93% of its 2017 sales from the U.S. healthcare system. While Endo's management, operations, and customers are almost exclusively U.S.–based, in 2013 Endo executed a corporate tax inversion to Ireland to avoid U.S. corporate taxes on their U.S. drug sales, and to avail of Ireland's corporate tax system. History and Acquisitions Endo was created as a result of a management buyout from DuPont Merck in 1997 led by Carol Ammon. In 2009, Endo bought Indevus Pharmaceuticals to diversify into endocrinology and oncology. The company entered the male hypogonadism market later in 2010 with Fortesta 2% gel. In November 2013, Endo agreed to purchase Paladin Labs Inc for about $1.6 billion to gain access to the Canadian market as well as expand into emerging markets. Endo used the 2013 acquisition of Paladin Labs, and Canadian tax laws, to execute a corp ...
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Hoechst Marion Roussel
Hoechst AG () was a German chemicals then life-sciences company that became Aventis Deutschland after its merger with France's Rhône-Poulenc S.A. in 1999. With the new company's 2004 merger with Sanofi-Synthélabo, it became a subsidiary of the resulting Sanofi-Aventis pharmaceuticals group. History The company was founded in 1863 as "Teerfarbenfabrik Meister, Lucius & Co." in Höchst, near Frankfurt and changed its name some years later to "Teerfarbenfabrik Meister Lucius & Brüning". In 1880 it became a stock company "Farbwerke vorm. Meister Lucius & Brüning AG". For the international market the name was simplified to "Farbwerke Hoechst AG". Until 1925 the Hoechst AG was independent. In 1916, the Hoechst AG was one of the co-founders of IG Farben, an advocacy group of Germany's chemicals industry to gain industrial power during and after World War I. In 1925, IG Farben turned from an advocacy group into the well-known conglomerate. World War II Various Hoechst faciliti ...
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Antitrust
Competition law is the field of law that promotes or seeks to maintain market competition by regulating anti-competitive conduct by companies. Competition law is implemented through public and private enforcement. It is also known as antitrust law (or just antitrust), anti-monopoly law, and trade practices law. The history of competition law reaches back to the Roman Empire. The business practices of market traders, guilds and governments have always been subject to scrutiny, and sometimes severe sanctions. Since the 20th century, competition law has become global. The two largest and most influential systems of competition regulation are United States antitrust law and European Union competition law. National and regional competition authorities across the world have formed international support and enforcement networks. Modern competition law has historically evolved on a national level to promote and maintain fair competition in markets principally within the territorial boun ...
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Federal Trade Commission
The Federal Trade Commission (FTC) is an independent agency of the United States government whose principal mission is the enforcement of civil (non-criminal) antitrust law and the promotion of consumer protection. The FTC shares jurisdiction over federal civil antitrust enforcement with the Department of Justice Antitrust Division. The agency is headquartered in the Federal Trade Commission Building in Washington, DC. The FTC was established in 1914 with the passage of the Federal Trade Commission Act, signed in response to the 19th-century monopolistic trust crisis. Since its inception, the FTC has enforced the provisions of the Clayton Act, a key antitrust statute, as well as the provisions of the FTC Act, et seq. Over time, the FTC has been delegated with the enforcement of additional business regulation statutes and has promulgated a number of regulations (codified in Title 16 of the Code of Federal Regulations). The broad statutory authority granted to the FTC prov ...
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