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Cericlamine Synthesis
Cericlamine (INN; developmental code JO-1017) is a potent and moderately selective serotonin reuptake inhibitor (SSRI) of the amphetamine family (specifically, a derivative of phentermine, and closely related to chlorphentermine, a highly selective serotonin releasing agent) that was investigated as an antidepressant for the treatment of depression, anxiety disorders, and anorexia nervosa by Jouveinal but did not complete development and was never marketed. It reached phase III clinical trials in 1996 before development was discontinued in 1999. Synthesis Arylation of methacrylic acid with a diazonium salt of 3,4-dichloroaniline (or 3,4-dichloro-benzenediazonium salt), is carried out according to the Meerwein reaction catalysed by a metallic halide. For the next step, the halide is displaced by dimethylamine, then esterification is performed, followed by reduction with a metal hydride. See also * 3,4-Dichloroamphetamine * Alaproclate * Bupropion * Chlorphentermine * ...
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Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ...
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3,4-dichloroaniline
Dichloroanilines are chemical compounds which consist of an aniline ring substituted with two chlorine atoms and have the molecular formula C6H5Cl2N. There are six isomers, varying in the positions of the chlorine atoms around the ring relative to the amino group. As aniline derivatives, they are named with the amino group in position 1. They are all colorless, although commercial samples can appear colored due to the presence of impurities. Several derivatives are used in the production of dyes and herbicides.Thomas Kahl, Kai-Wilfrid Schröder, F. R. Lawrence, W. J. Marshall, Hartmut Höke, Rudolf Jäckh "Aniline" in ''Ullmann's Encyclopedia of Industrial Chemistry'', 2007; John Wiley & Sons: New York. {, class="wikitable" , +Dichloroaniline isomers , - ! Compound name !! CAS# !! Chemical structure !! Melting point , - , 2,3-Dichloroaniline , , 608-27-5 , , , , , - , 2,4-Dichloroaniline , , 554-00-7 , , , , , - , 2,5-Dichloroaniline , , 95-82-9 , , , , , - , ...
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Omiloxetine
Omiloxetine (omiloextinum, omiloxetino INN) was a selective serotonin reuptake inhibitor drug candidate that underwent preclinical development by the Spanish pharmaceutical company, Ferrer Internacional, until 2005, when it was abandoned. Rafael Foguet also patented Abaperidone. References 4-Phenylpiperidines Benzodioxoles Ketones Fluoroarenes Phenethylamines Selective serotonin reuptake inhibitors {{nervous-system-drug-stub ...
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Methylenedioxyphentermine
3,4-Methylenedioxyphentermine (MDPH) is a lesser-known psychedelic drug. MDPH was first synthesized by Alexander Shulgin. In his book '' PiHKAL (Phenethylamines i Have Known And Loved)'', the dosage range is listed as 160–240 mg, and the duration as 3–5 hours. MDPH's effects are very similar to those of MDA: they both are smooth and "stoning," and do not cause any visuals. They also alter dreams and dream patterns. Shulgin describes MDPH as a promoter; it promotes the effects of other drugs, similarly to 2C-D. Very little data exists about the pharmacological properties, metabolism, and toxicity of MDPH. Legality United Kingdom This substance is a Class A drug in the Drugs controlled by the UK Misuse of Drugs Act. See also * 3,4-Dichloroamphetamine * Cericlamine * Chlorphentermine * Cloforex * Clortermine * Etolorex * Phentermine Phentermine ( phenyl- tertiary-butyl amine), with several brand names including Ionamin and Sentis, is a medication used together w ...
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Indalpine
Indalpine ( INN, BAN; brand name Upstène; developmental code name LM-5008) is a selective serotonin reuptake inhibitor (SSRI) class drug that was briefly marketed. It was discovered in 1977 by the pharmacologists Le Fur and Uzan at Pharmuka, a small French pharmaceutical firm, who credit Baron Shopsin and his colleagues at NYU-Bellevue/NYU School of Medicine in New York with providing the basis for their work. They were particularly influenced by the series of "synthesis inhibitor studies" carried out by Shopsin's team during the early to mid 1970s, and in particular, the clinical report by Shopsin et al. (1976) relating to PCPA's rapid reversal of antidepressant response to tranylcypromine in depressed patients. This led to an understanding of the role of the monoamine neurotransmitter serotonin (5-hydroxytryptamine, or 5HT) in the therapeutic effects of the available tricyclic and MAOI class antidepressants. The studies led to widespread recognition of a serotonin hypoth ...
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Ifoxetine
Ifoxetine (CGP-15,210-G) is a selective serotonin reuptake inhibitor (SSRI) which was investigated as an antidepressant in the 1980s but was never marketed. Ifoxetine selectively blocks the reuptake of serotonin in the brain supposedly without affecting it in the periphery. Supporting this claim, ifoxetine was found to be efficacious in clinical trials and was very well tolerated, producing almost no physical Physical may refer to: *Physical examination In a physical examination, medical examination, or clinical examination, a medical practitioner examines a patient for any possible medical signs or symptoms of a medical condition. It generally co ... side effects or other complaints of significant concern. References Secondary alcohols Antidepressants Phenol ethers Piperidines Selective serotonin reuptake inhibitors {{nervous-system-drug-stub ...
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Femoxetine
Femoxetine ( INN; tentative brand name Malexil; developmental code name FG-4963) is a drug related to paroxetine that was being developed as an antidepressant by Danish pharmaceutical company Ferrosan in 1975 before acquisition of the company by Novo Nordisk. It acts as a selective serotonin reuptake inhibitor (SSRI). Development was halted to focus attention on paroxetine instead, as femoxetine could not be administered as a daily pill. Both femoxetine and paroxetine were invented in the 1970s. Jørgen Anders Christensen's name is on the patents and Jorgen Buus-Lassen's name is on the pharmacology paper. After Ferrosan's acquisition, femoxetine died from neglect. In a separate patent, Ferrosan stated that Femoxetine could be used as an appetite suppressant, using ten times the dosage than for paroxetine, 300 - 400mg daily. Femoxetine has the same stereochemical properties as Nocaine, another agent with a similar structure claimed to have been synthesized using arecoline ...
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Etolorex
Etolorex is an anorectic of the amphetamine class. It was never marketed. Synthesis Made by the reaction of chlorphentermine with 2-Chloroethanol. See also * 3,4-Dichloroamphetamine * Cericlamine * Chlorphentermine * Cloforex * Clortermine * Methylenedioxyphentermine * Phentermine Phentermine ( phenyl- tertiary-butyl amine), with several brand names including Ionamin and Sentis, is a medication used together with diet and exercise to treat obesity. It is taken by mouth for up to a few weeks at a time, after which the ben ... References Primary alcohols Substituted amphetamines Anorectics Chloroarenes Monoamine releasing agents Abandoned drugs {{nervous-system-drug-stub ...
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Cloforex
Cloforex (Oberex) is an anorectic of the amphetamine class. It is a prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ... to chlorphentermine. It never became a mass produced drug in part due to the side effects found in mice. Mice who consumed 75 mg of cloforex a day experienced weight loss along with pulmonary hypertension and hair loss. References Anorectics Substituted amphetamines Carbamates Chloroarenes Prodrugs Serotonin receptor agonists Serotonin releasing agents {{nervous-system-drug-stub ...
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Clortermine
Clortermine (Voranil) was developed by Ciba in the 1960s and is an anorectic drug of the amphetamine class. It is the 2-chloro analogue of the better known appetite suppressant phentermine, and is the 2-chloro positional isomer of chlorphentermine. Clortermine produces very low rates of self-administration in animals similarly to chlorphentermine, and as a result it likely does not act on dopamine. Instead, it may act as a serotonin and/or norepinephrine releasing agent. See also * 3,4-Dichloroamphetamine * Cericlamine * Chlorphentermine * Cloforex * Etolorex * Methylenedioxyphentermine * Phentermine Phentermine ( phenyl- tertiary-butyl amine), with several brand names including Ionamin and Sentis, is a medication used together with diet and exercise to treat obesity. It is taken by mouth for up to a few weeks at a time, after which the ben ... References Anorectics Chloroarenes Monoamine releasing agents Substituted amphetamines {{Nervous-system-drug ...
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Chlorphentermine
Chlorphentermine (trade names Apsedon, Desopimon, Lucofen) is a serotonergic appetite suppressant of the amphetamine family. Developed in 1962, it is the 4-chloro derivative of the better known appetite suppressant phentermine, which is still in current use. Chlorphentermine acts as a highly selective serotonin releasing agent (SRA). It is not a psychostimulant and has little or no abuse potential, but is classed as a Schedule III drug in the USA due mainly to its similarity to other appetite suppressants such as diethylpropion which have been more widely abused. It is no longer used due mainly to safety concerns, as it has a serotonergic effects profile similar to other withdrawn appetite suppressants such as fenfluramine and aminorex which were found to cause pulmonary hypertension and cardiac fibrosis following prolonged use. The plasma half-life is about five days. It was withdrawn from the market in the UK in 1974. See also * Aminorex * Cericlamine * Cloforex ...
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Bupropion
Bupropion, sold under the brand names Wellbutrin and Zyban among others, is an atypical antidepressant primarily used to treat major depressive disorder and to support smoking cessation. It is also popular as an add-on medication in the cases of "incomplete response" to the first-line selective serotonin reuptake inhibitor (SSRI) antidepressant. Bupropion has several features that distinguish it from other antidepressants: it does not usually cause sexual dysfunction; it is not associated with weight gain and sleepiness, and it is more effective than SSRIs at improving symptoms of hypersomnia and fatigue. Bupropion does, however, carry a much higher risk of seizure than many other antidepressants and extreme caution must be taken in patients with a history of seizure disorder. Common adverse effects of bupropion with the greatest difference from placebo are dry mouth, nausea, constipation, insomnia, anxiety, tremor, and excessive sweating. Raised blood pressure is notable. ...
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