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Ticlopidine
Ticlopidine, sold under the brand name Ticlid, is a medication used to reduce the risk of thrombotic strokes. It is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor. Research initially showed that it was useful for preventing strokes and coronary stent occlusions. However, because of its rare but serious side effects of neutropenia and thrombotic thrombocytopenic purpura it was primarily used in patients in whom aspirin was not tolerated, or in whom dual antiplatelet therapy was desirable. With the advent of newer and safer antiplatelet drugs such as clopidogrel and ticagrelor, its use remained limited. It was patented in 1973 and approved for medical use in 1978. Medical uses Ticlopidine is Indication (medicine), indicated for the prevention of strokes and when combined with aspirin, for people with a new coronary stent to prevent closure. Stroke Ticlopidine is considered a second-line option for the prevention o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYP2D6 Inhibitors
Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the ''CYP2D6'' gene. ''CYP2D6'' is primarily expressed in the liver. It is also highly expressed in areas of the central nervous system, including the substantia nigra. CYP2D6, a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. In particular, CYP2D6 is responsible for the metabolism and clearance (medicine), elimination of approximately 25% of clinically used drugs, via the addition or removal of certain functional groups – specifically, hydroxylation, demethylation, and dealkylation. CYP2D6 also activates some prodrugs. This enzyme also metabolizes several endogenous substances, such as serotonin, hydroxytryptamines, neurosteroids, and both m-tyramine, ''m''-tyramine and tyramine, ''p''-tyramine which CYP2D6 metabolizes into dopamine in the brain and liver. Considerable variation exists in the effic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thienopyridine
Thienopyridines are a class of selective, reversible ADP receptor/P2Y12 inhibitors used for their anti-platelet activity. Examples Drugs in this class include: clopidogrel (Plavix), prasugrel (Effient), and ticlopidine (Ticlid). Tinoridine was actually a predecessor to this work. Alternatives Ticagrelor Ticagrelor, sold under the brand name Brilinta among others, is a medication used for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries. It ... (Brilinta) is often listed with thienopyridine inhibitors and has similar indications for use but is not a thienopyridine. It is a cyclo-pentyltriazolo-pyrimidine that reversibly inhibits the P2Y12 receptor. References {{Blood-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thrombotic Thrombocytopenic Purpura
Thrombotic thrombocytopenic purpura (TTP) is a blood disorder that results in blood clots forming in small blood vessels throughout the body. This results in a low platelet count, low red blood cells due to their breakdown, and often kidney, heart, and brain dysfunction. Symptoms may include large bruises, fever, weakness, shortness of breath, confusion, and headache. Repeated episodes may occur. In about half of cases a trigger is identified, while in the remainder the cause remains unknown. Known triggers include bacterial infections, certain medications, autoimmune diseases such as lupus, and pregnancy. The underlying mechanism typically involves antibodies inhibiting the enzyme ADAMTS13. This results in decreased break down of large multimers of von Willebrand factor (vWF) into smaller units. Less commonly TTP is inherited from a person's parents, known as Upshaw–Schulman syndrome, such that ADAMTS13 dysfunction is present from birth. Diagnosis is typically based on sym ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ticagrelor
Ticagrelor, sold under the brand name Brilinta among others, is a medication used for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries. It acts as a platelet aggregation inhibitor by antagonising the P2Y12 receptor. The drug is produced by AstraZeneca. The most common side effects include dyspnea (difficulty breathing), bleeding and raised uric acid level in the blood. It was approved for medical use in the European Union in December 2010, and in the United States in July 2011. In 2020, it was the 247th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses In the US, ticagrelor is indicated to reduce the risk of stroke in people with acute ischemic stroke or high-risk transient ischemic attack. In the EU, ticagrelor, co-administered with acetylsalicylic acid (aspirin), is indicated for the prevention of atherothrom ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ADP Receptor
P2Y receptors are a family of purinergic G protein-coupled receptors, stimulated by nucleotides such as adenosine triphosphate, adenosine diphosphate, uridine triphosphate, uridine diphosphate and UDP-glucose.To date, 8 P2Y receptors have been cloned in humans: P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13 and P2Y14. P2Y receptors are present in almost all human tissues where they exert various biological functions based on their G-protein coupling. P2Y receptors mediate responses including vasodilation, blood clotting, and immune response. Due to their ubiquity and variety in function, they are a common biological target in pharmacological development. Structure P2Y receptors are membrane proteins belonging to the class A family of G protein-coupled receptors (GPCRs). P2Y receptor proteins display large-scale structural domains typical of GPCRs, consisting of seven hydrophobic transmembrane helices connected by three short extracellular loops and three variably siz ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as haloarene) is an aromatic compound in which one or more hydrogen atoms, directly bonded to an aromatic ring are replaced by a halide. The haloarene are different from haloalkanes because they exhibit many differences in methods of preparation and properties. The most important members are the aryl chlorides, but the class of compounds is so broad that there are many derivatives and applications. Preparation The two main preparatory routes to aryl halides are direct halogenation and via diazonium salts. Direct halogenation In the Friedel-Crafts halogenation, Lewis acids serve as catalysts. Many metal chlorides are used, examples include iron(III) chloride or aluminium chloride. The most important aryl halide, chlorobenzene is produced by this route. Monochlorination of benzene is always accompanied by formation of the dichlorobenzene derivatives. Arenes with electron donating groups react with halogens even in the absence of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine Diphosphate Receptor Inhibitors
Adenosine (symbol A) is an organic compound that occurs widely in nature in the form of diverse derivatives. The molecule consists of an adenine attached to a ribose via a β-N9-glycosidic bond. Adenosine is one of the four nucleoside building blocks of RNA (and its derivative deoxyadenosine is a building block of DNA), which are essential for all life. Its derivatives include the energy carriers adenosine mono-, di-, and triphosphate, also known as AMP/ADP/ATP. Cyclic adenosine monophosphate (cAMP) is pervasive in signal transduction. Adenosine is used as an intravenous medication for some cardiac arrhythmias. Adenosyl (abbreviated Ado or 5'-dAdo) is the chemical group formed by removal of the 5′-hydroxy (OH) group. It is found in adenosylcobalamin (an active form of vitamin B12) and as a radical in radical SAM enzymes. Medical uses Supraventricular tachycardia In individuals with supraventricular tachycardia (SVT), adenosine is used to help identify and convert the rhyt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
The New York Times
''The New York Times'' (''the Times'', ''NYT'', or the Gray Lady) is a daily newspaper based in New York City with a worldwide readership reported in 2020 to comprise a declining 840,000 paid print subscribers, and a growing 6 million paid digital subscribers. It also is a producer of popular podcasts such as '' The Daily''. Founded in 1851 by Henry Jarvis Raymond and George Jones, it was initially published by Raymond, Jones & Company. The ''Times'' has won 132 Pulitzer Prizes, the most of any newspaper, and has long been regarded as a national " newspaper of record". For print it is ranked 18th in the world by circulation and 3rd in the U.S. The paper is owned by the New York Times Company, which is publicly traded. It has been governed by the Sulzberger family since 1896, through a dual-class share structure after its shares became publicly traded. A. G. Sulzberger, the paper's publisher and the company's chairman, is the fifth generation of the family to head the pa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hoffmann-La Roche
F. Hoffmann-La Roche AG, commonly known as Roche, is a Swiss multinational healthcare company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX Swiss Exchange. The company headquarters are located in Basel. Roche is the fifth largest pharmaceutical company in the world by revenue, and the leading provider of cancer treatments globally. The company controls the American biotechnology company Genentech, which is a wholly owned affiliate, and the Japanese biotechnology company Chugai Pharmaceuticals, as well as the United States-based companies Ventana and Foundation Medicine. Roche's revenues during fiscal year 2020 were 58.32 billion Swiss francs. Descendants of the founding Hoffmann and Oeri families own slightly over half of the bearer shares with voting rights (a pool of family shareholders 45%, and Maja Oeri a further 5% apart), with Swiss pharma firm Novartis owning a furth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Syntex
Laboratorios Syntex SA (later Syntex Laboratories, Inc.) was a pharmaceutical company formed in Mexico City in January 1944 by Russell Marker, Emeric Somlo, and Federico Lehmann to manufacture therapeutic steroids from the Mexican yams called ''cabeza de negro'' (''Dioscorea mexicana'') and ''Barbasco'' (''Dioscorea composita''). The demand for barbasco by Syntex initiated the Mexican barbasco trade. As the American Chemistry Society later explained: “In early 1944, the new Mexican company was chartered and named Syntex, S.A. (‘Synthesis and Mexico’). Russell Marker, shortly thereafter, left Syntex on account of his ruthless cofounder. Luis E. Miramontes, George Rosenkranz and Carl Djerassi's successful synthesis of norethindrone (also known as norethindrone) — which was later proven to be an effective pregnancy inhibitor — led to an infusion of capital into Syntex and the Mexican steroid pharmaceutical industry. George Rosenkranz and Carl Djerassi went on to synthesize ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sanofi
Sanofi S.A. is a French multinational pharmaceutical and healthcare company headquartered in Paris, France. Originally, the corporation was established in 1973 and merged with Synthélabo in 1999 to form Sanofi-Synthélabo. In 2004, Sanofi-Synthélabo merged with Aventis and renamed to Sanofi-Aventis, which were each the product of several previous mergers. It changed its name back to Sanofi in May 2011. The company is a component of the Euro Stoxx 50 stock market index. Sanofi engages in the research and development, manufacturing and marketing of pharmaceutical drugs principally in the prescription market, but the firm also develops over-the-counter medication. The corporation covers seven major therapeutic areas: cardiovascular, central nervous system, diabetes, internal medicine, oncology, thrombosis and vaccines (it is the world's largest producer of the latter through its subsidiary Sanofi Pasteur). History Sanofi-Synthélabo Sanofi was founded in 1973 as a subsidia ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Discovery
In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered by identifying the active ingredient from traditional remedies or by serendipitous discovery, as with penicillin. More recently, chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that had a desirable therapeutic effect in a process known as classical pharmacology. After sequencing of the human genome allowed rapid cloning and synthesis of large quantities of purified proteins, it has become common practice to use high throughput screening of large compounds libraries against isolated biological targets which are hypothesized to be disease-modifying in a process known as reverse pharmacology. Hits from these screens are then tested in cells and then in animals for efficacy. Modern drug discovery involves the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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