Nariman Bomanshaw Mehta, was an Indian-born American organic chemist and pharmacologist who designed, synthesized, and patented which organic compound, medication primarily used as an antidepressant and smoking cessation aid?
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Nariman Mehta Nariman Bomanshaw Mehta (April 8, 1920 – August 22, 2014) was an Indian-born American organic chemist and pharmacologist who designed, synthesized, and patented the organic compound Bupropion, marketed under the name Wellbutrin as an antidepressant and smoking cessation aid.
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Bupropion Bupropion is a medication primarily used as an antidepressant and smoking cessation aid. It is marketed as Wellbutrin and Zyban among other trade names. It is one of the most frequently prescribed antidepressants in the United States and Canada, although in many countries this is an off-label use. It is an effective antidepressant on its own, but is also popular as an add-on medication in cases of incomplete response to first-line SSRI antidepressants. Bupropion is taken in tablet form and is available only by prescription in most countries.
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Phthalazine Phthalazine, also called benzo-orthodiazine or benzopyridazine, is a heterocyclic organic compound with the molecular formula CHN. It is isomeric with other naphthyridines including quinoxaline, cinnoline and quinazoline.
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Phenothiazine Phenothiazine, abbreviated PTZ, is an organic compound that has the formula S(CH)NH and is related to the thiazine-class of heterocyclic compounds. Although the parent compound has no uses, derivatives of phenothiazine are highly bioactive and have widespread use and rich history. The derivative chlorpromazine revolutionized the field of psychiatry and allergy treatment. An earlier derivative, methylene blue, was one of the first antimalarial drugs, and as of 2015 derivatives are under investigation as possible anti-infective drugs. Phenothiazine is a prototypical pharmaceutical lead structure in medicinal chemistry.
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Pyrazolopyrimidine Pyrazolopyrimidines are a series of isomeric heterocyclic chemical compounds with the molecular formula CHN. They form the central core of a variety of more complex chemical compounds including some pharmaceuticals and pesticides.
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Naphthalene Naphthalene is an organic compound with formula C10H8 . It is the simplest polycyclic aromatic hydrocarbon, and is a white crystalline solid with a characteristic odor that is detectable at concentrations as low as 0.08 ppm by mass. As an aromatic hydrocarbon, naphthalene's structure consists of a fused pair of benzene rings. It is best known as the main ingredient of traditional mothballs.
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Cinitapride Cinitapride (trade names Cintapro, Pemix) is a gastroprokinetic agent and antiulcer agent of the benzamide class which is marketed in India, Mexico, Pakistan and Spain. It acts as an agonist of the 5-HT and 5-HT receptors and as an antagonist of the 5-HT receptors.
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Acetylcholinesterase inhibitor An acetylcholinesterase inhibitor (often abbreviated AChEI) or anti-cholinesterase is a chemical or a drug that inhibits the acetylcholinesterase enzyme from breaking down acetylcholine, thereby increasing both the level and duration of action of the neurotransmitter acetylcholine. Acetylcholinesterase inhibitors are classified as reversible, irreversible, or quasi-irreversible (also called pseudo-irreversible).
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EMDT 2-Ethyl-5-methoxy-"N","N"-dimethyltryptamine (EMDT) is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT receptor agonist, with a K of 16 nM, and was one of the first selective agonists developed for this receptor. EMDT inhibits both short- and long-term memory formation in animal studies, and this effect can be reversed by the selective 5-HT antagonist SB-399,885. Additionally, it is active in the tail suspension test, suggesting that it could be an effective antidepressant.
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Anandamide Anandamide, also known as "N"-arachidonoylethanolamine or AEA, is a fatty acid neurotransmitter derived from the non-oxidative metabolism of eicosatetraenoic acid (arachidonic acid) an essential ω-6 polyunsaturated fatty acid. The name is taken from the Sanskrit & Pāli word "ananda", which means "joy, bliss, delight", and amide. It is synthesized from "N"-arachidonoyl phosphatidylethanolamine by multiple pathways. It is degraded primarily by the fatty acid amide hydrolase (FAAH) enzyme, which converts anandamide into ethanolamine and arachidonic acid. As such, inhibitors of FAAH lead to elevated anandamide levels and are being pursued for therapeutic use.
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Sazetidine A Sazetidine A (AMOP-H-OH) is a drug which acts as a subtype selective partial agonist at α4β2 neural nicotinic acetylcholine receptors, acting as an agonist at (α4)2(β2)3 pentamers, but as an antagonist at (α4)3(β2)2 pentamers. It has potent analgesic effects in animal studies comparable to those of epibatidine, but with less toxicity, and also has antidepressant action.
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Tizanidine Tizanidine (trade names Zanaflex (Acorda Therapeutics), Sirdalud (Novartis), Relentus (Beximco Pharma) is a drug that is used as a muscle relaxant. It is a centrally acting α adrenergic agonist. It is used to treat the spasms, cramping, and tightness of muscles caused by medical problems such as multiple sclerosis, ALS, spastic diplegia, back pain, or certain other injuries to the spine or central nervous system. It is also prescribed off-label for migraine headaches, as a sleep aid, and as an anticonvulsant. It is also prescribed for some symptoms of fibromyalgia.
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Sho-saiko-to Sho-Saiko-To or SST (), also known as Minor Bupuleurum Formula and "Xiao Chai Hu Tang" in Chinese小柴胡汤, is a herbal supplement, believed to enhance liver health. Sho-Saiko-To is a widely used prescription drug in China and is a listed formula in China. There are currently ongoing clinical trials for Sho-Saiko-To at University of California, San Diego and Memorial Sloan-Kettering Cancer Center. The active ingredients of Sho-Saiko-To discovered so far include: Baicalin, Baicalein, Glycyrrhizin, Saikosaponins, Ginsenosides, Wogonin, Gingerol.
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Cotinine Cotinine is an alkaloid found in tobacco and is also the predominant metabolite of nicotine. Cotinine is used as a biomarker for exposure to tobacco smoke. Cotinine is currently being studied as a treatment for depression, PTSD, schizophrenia, Alzheimer's disease and Parkinson's disease. Cotinine was developed as an antidepressant as a fumaric acid salt, cotinine fumarate, to be sold under the brand name Scotine but it was never marketed.
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Methoxypiperamide Methoxypiperamide (also known as MeOP and MEXP) is a psychoactive drug of the piperazine class that has been sold online as a designer drug. It is the 4-methoxy-α-keto analog of methylbenzylpiperazine.
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Mirtazapine Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant which is used primarily in the treatment of depression. In addition to its antidepressant properties, mirtazapine has anxiolytic, sedative, antiemetic, and appetite stimulant effects and is sometimes used in the treatment of anxiety disorders, insomnia, nausea and vomiting, and to produce weight gain when desirable. It is taken by mouth.
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Amitriptylinoxide Amitriptylinoxide (brand names Amioxid, Ambivalon, Equilibrin), or amitriptyline "N"-oxide, is a tricyclic antidepressant (TCA) which was introduced in Europe in the 1970s for the treatment of depression.
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Piperoxan Piperoxan, also known as benodaine, is a drug which was the very first antihistamine to be discovered. This compound, derived from benzodioxan, was prepared in the early 1930s by Daniel Bovet and Ernest Fourneau at the Pasteur Institute in France. Formerly investigated by Fourneau as an α-adrenergic-blocking agent, they demonstrated that it also antagonized histamine-induced bronchospasm in guinea pigs, and published their findings in 1933. Bovet went on to win the 1957 Nobel Prize in Physiology or Medicine for his contribution, and one of their students, Anne-Marie Staub, published the first structure-activity relationship (SAR) study of antihistamines in 1939.
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Organic chemistry Organic chemistry is a chemistry subdiscipline involving the scientific study of the structure, properties, and reactions of organic compounds and organic materials, i.e., matter in its various forms that contain carbon atoms. Study of structure includes many physical and chemical methods to determine the chemical composition and the chemical constitution of organic compounds and materials. Study of properties includes both physical properties and chemical properties, and uses similar methods as well as methods to evaluate chemical reactivity, with the aim to understand the behavior of the organic matter in its pure form (when possible), but also in solutions, mixtures, and fabricated forms. The study of organic reactions includes probing their scope through use in preparation of target compounds (e.g., natural products, drugs, polymers, etc.) by chemical synthesis, as well as the focused study of the reactivities of individual organic molecules, both in the laboratory and via theoretical (in silico) study.
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Phenoxypropazine Phenoxypropazine (trade name Drazine) is an irreversible and non-selective monoamine oxidase inhibitor (MAOI) of the hydrazine family. It was introduced as an antidepressant in 1961, but was subsequently withdrawn in 1966 due to hepatotoxicity concerns.
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RS-102221 RS-102221 is a drug developed by Hoffmann–La Roche, which was one of the first compounds discovered that acts as a potent and selective antagonist at the serotonin 5-HT receptor, with around 100x selectivity over the closely related 5-HT and 5-HT receptors. It has anxiolytic effects in animal studies, increases the effectiveness of SSRI antidepressants, and shows a complex interaction with cocaine, increasing some effects but decreasing others, reflecting a role for the 5-HT receptor in regulation of the dopamine signalling system in the brain.
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Sulfonylurea Sulfonylureas (UK: sulphonylurea) are a class of organic compounds used in medicine and agriculture. They are antidiabetic drugs widely used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta cells in the pancreas. A number of sulfonylureas are also used as herbicides ("weedkiller"), because they can interfere with plant biosynthesis of certain amino acids. Sulfonylureas are also used experimentally to inhibit interleukin 1 beta release from the NALP3 (or NLRP3) inflammasome.