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Surinabant 3D Spacefill
Surinabant
Surinabant
(SR147778) is a cannabinoid receptor type 1 antagonist developed by Sanofi-Aventis.[1] It is being investigated as a potential treatment for nicotine addiction, to assist smoking cessation. It may also be developed as an anorectic drug to assist with weight loss, however there are already several CB1 antagonists or inverse agonists on the market or under development for this application,[2] so surinabant is at present mainly being developed as an anti-smoking drug,[3] with possible application in the treatment of other addictive disorders such as alcoholism.[4][5] Other potential applications such as treatment of ADHD
ADHD
have also been proposed.[6] A dose ranging study was done for smoking cessation[7] in 2012; it did not improve success rate, but reduced weight gain
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Anatomical Therapeutic Chemical Classification System
The Anatomical Therapeutic
Therapeutic
Chemical (ATC) Classification System
System
is used for the classification of active ingredients of drugs according to the organ or system on which they act and their therapeutic, pharmacological and chemical properties. It is controlled by the World Health Organization Collaborating Centre for Drug
Drug
Statistics Methodology (WHOCC), and was first published in 1976.[1] This pharmaceutical coding system divides drugs into different groups according to the organ or system on which they act or their therapeutic and chemical characteristics. Each bottom-level ATC code stands for a pharmaceutically used substance, or a combination of substances, in a single indication (or use)
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Hydrogen Cyanamide
Cyanamide
Cyanamide
is an organic compound with the formula CN2H2. This white solid is widely used in agriculture and the production of pharmaceuticals and other organic compounds. It is also used as an alcohol-deterrent drug in Canada, Europe and Japan.[citation needed] The molecule features a nitrile group attached to an amino group. Derivatives of this compound are also referred to as cyanamides, the most common being calcium cyanamide (CaCN2).Contents1 Tautomers and self-condensations 2 Production 3 Reactions and uses3.1 Agricultural use4 Environmental aspects 5 Safety 6 References 7 External linksTautomers and self-condensations[edit] Containing both a nucleophilic and electrophilic site within the same molecule, cyanamide undergoes various reactions with itself. Cyanamide exists as two tautomers, one with the connectivity N≡C–NH2 and the other with the formula HN=C=NH ("carbodiimide" tautomer)
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Cytisine
Cytisine, also known as baptitoxine and sophorine, is an alkaloid that occurs naturally in several plant genera, such as Laburnum
Laburnum
and Cytisus of the family Fabaceae. It has been used medically to help with smoking cessation.[1] Its molecular structure has some similarity to that of nicotine and it has similar pharmacological effects. Like varenicline, cytisine is a partial agonist of nicotinic acetylcholine receptors (nAChRs). Cytisine
Cytisine
has a short half-life of 4.8 hours,[2] and is rapidly eliminated from the body
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Lobeline
Lobeline
Lobeline
is an alkaloid found in a variety of plants, particularly those in the genus Lobelia, including Indian tobacco (Lobelia inflata), Devil's tobacco ( Lobelia
Lobelia
tupa), cardinal flower (Lobelia cardinalis), great lobelia ( Lobelia
Lobelia
siphilitica), Lobelia
Lobelia
chinensis, and Hippobroma longiflora
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Mecamylamine
Mecamylamine
Mecamylamine
(INN, BAN; or mecamylamine hydrochloride (USAN); brand names Inversine, Vecamyl[1]) is a non-selective, non-competitive antagonist of the nicotinic acetylcholine receptors (nAChRs) that was introduced in the 1950s as an antihypertensive drug.[2] In the United States, it was voluntarily withdrawn from the market in 2009 but was brought to market in 2013 as Vecamyl and eventually was marketed by Turing Pharmaceuticals.[3][4] Chemically, mecamylamine is a secondary aliphatic amine, with a pKaH of 11.2[5]Contents1 Pharmacology and clinical applications 2 Toxicology
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Varenicline
Varenicline
Varenicline
(trade name Chantix and Champix), is a prescription medication used to treat nicotine addiction
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Adrenergic Agonist
An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of adrenergic receptors are: α1, α2, β1, β2, and β3, although there are more subtypes, and agonists vary in specificity between these receptors, and may be classified respectively. However, there are also other mechanisms of adrenergic agonism. Epinephrine
Epinephrine
and norepinephrine are endogenous and broad-spectrum. More selective agonists are more useful in pharmacology. An adrenergic agent is a drug, or other substance, which has effects similar to, or the same as, epinephrine (adrenaline). Thus, it is a kind of sympathomimetic agent
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Clonidine
Clonidine
Clonidine
(trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions.[4] It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist that has been in clinical use since 1966.[5][6]Contents1 Medical uses1.1
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Alcohol Dependence
Alcohol dependence
Alcohol dependence
is a previous psychiatric diagnosis in which an individual is physically or psychologically dependent upon alcohol (also known formally as ethanol)
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Acetaldehyde Dehydrogenase Inhibitor
A disulfiram-like drug is a drug that causes hypersensitivity to the unpleasant and toxic effects of alcohol.[1][2] Such effects may include nausea, vomiting, flushing, dizziness, throbbing headache, chest and abdominal discomfort, and general hangover-like symptoms among others.[1][2] They are caused by accumulation of acetaldehyde, a major but toxic metabolite of alcohol formed by the enzyme alcohol dehydrogenase.[1][2] The reaction has been variously termed a disulfiram-like reaction, alcohol intolerance, and acetaldehyde syndrome.[3] The prototypical drug of this group is disulfiram (brand name Antabuse), which acts as an acetaldehyde dehydrogenase inhibitor, preventing the metabolism of acetaldehyde into acetic acid, and is used in the treatment of alcoholism.[1][2] A variety of other drugs cause disulfiram-like reactions upon consumption of alcohol as unintended drug interactions and side effects.[1][2] Many disulfiram-like drugs act as inhibitors of acetaldehyde dehydrogenase si
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Disulfiram
Disulfiram
Disulfiram
(sold under the trade names Antabuse and Antabus) is a drug used to support the treatment of chronic alcoholism by producing an acute sensitivity to ethanol (drinking alcohol). Disulfiram
Disulfiram
works by inhibiting the enzyme acetaldehyde dehydrogenase, which means that many of the effects of a "hangover" are felt immediately after alcohol is consumed. " Disulfiram
Disulfiram
plus alcohol, even small amounts, produce flushing, throbbing in head and neck, throbbing headache, respiratory difficulty, nausea, copious vomiting, sweating, thirst, chest pain, palpitation, dyspnea, hyperventilation, tachycardia, hypotension, syncope, marked uneasiness, weakness, vertigo, blurred vision, and confusion
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Calcium Carbimide
Calcium carbimide, sold as the citrate salt under the trade name Temposil, is a disulfiram-like drug. Its effects are similar to the drug disulfiram (Antabuse) in that it interferes with the normal metabolism of alcohol by preventing the breakdown of the metabolic byproduct acetaldehyde. The result is that when alcohol is consumed by users of calcium carbimide, they experience severe reactions which include symptoms such as sweating, difficulty breathing, rapid heartbeat, rash, nausea and vomiting, and headache. A recent 9-year study found that incorporation of supervised carbimide and the similar drug, disulfiram, into a comprehensive treatment program resulted in an abstinence rate of over 50%.[1] Temposil was developed by Drs. Ken Ferguson and Gordon Bell, who tested the drug on themselves.[2][3][4] It was patented in 1955 by the Alcoholism Research Foundation of Ontario.[5] See also[edit]AcamprosateReferences[edit]^ Krampe H, Stawicki S, Wagner T, et al. (January 2006)
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Acamprosate
Acamprosate, sold under the brand name Campral, is a medication used along with counselling to treat alcohol dependence.[1][2] Acamprosate
Acamprosate
is thought to stabilize chemical signaling in the brain that would otherwise be disrupted by alcohol withdrawal.[3] When used alone, acamprosate is not an effective therapy for alcoholism in most individuals;[4] however, studies have found that acamprosate works best when used in combination with psychosocial support since it facilitates a reduction in alcohol consumption as well as full abstinence.[2][5][6] Serious side effects include al
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Nicotine Dependence
Nicotine
Nicotine
dependence, or tobacco use disorder, is a state of dependence upon nicotine. There are different ways of measuring nicotine dependence.[citation needed] Some nicotine dependence assessments focus on key physical dependence outcomes like the development of tolerance which allows people to smoke heavily.[citation needed] Other assessments ask about psychosocial outcomes or underlying mechanisms of dependence.[citation needed] These different assessments either characterize dependence as a continuous construct or use cut-offs to diagnose whether or not a person is dependent.[citation needed] Nicotine
Nicotine
dependence is especially a concern among some populations such as those with co-occurring mental illness
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Opioid Antagonist
An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. Naloxone
Naloxone
and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to the opioid receptors with higher affinity than agonists but do not activate the receptors. This effectively blocks the receptor, preventing the body from responding to opioids and endorphins. Some opioid antagonists are not pure antagonists but do produce some weak opioid partial agonist effects, and can produce analgesic effects when administered in high doses to opioid-naive individuals. Examples of such compounds include nalorphine and levallorphan. However, the analgesic effects from these specific drugs are limited and tend to be accompanied by dysphoria, most likely due to additional agonist action at the κ-opioid receptor
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