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Tametraline
Tametraline (CP-24,441) is the parent of a series of chemical compounds investigated at Pfizer that eventually led to the development of sertraline. Sertraline has been called "3,4-dichloro-tametraline". This is correct but it is an oversimplification in the sense that sertraline is the ''S'',''S''-isomer whereas tametraline is the 1''R'',4''S''-stereoisomer. 1''R''-Methylamino-4''S''-phenyl-tetralin is a potent inhibitor of norepinephrine uptake in rat brain synaptosomes, reverses reserpine induced hypothermia in mice, and blocks uptake of 3H-Norepinephrine into rat heart. Tametraline is a norepinephrine–dopamine reuptake inhibitor. Indatraline is an indanamine homolog of tetralin-based tametraline, although in the case of indatraline the product is pm-dichlorinated. See also * Cyproheptadine * Dasotraline * Desmethylsertraline * EXP-561 (1-amino-4-phenylbicyclo .2.2ctane) * JNJ-7925476 * Lometraline * Nefopam * Sertraline Sertraline, sold under the brand name ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sertraline
Sertraline, sold under the brand name Zoloft among others, is an Antidepressant, antidepressant medication of the selective serotonin reuptake inhibitor (SSRI) class used to treat major depressive disorder, generalized anxiety disorder, social anxiety disorder, obsessive–compulsive disorder (OCD), panic disorder, and premenstrual dysphoric disorder. Although also having approval for post-traumatic stress disorder (PTSD), findings indicate it leads to only modest improvements in symptoms associated with this condition. The drug shares the common Side effect, side effects and contraindications of other SSRIs, with high rates of nausea, diarrhea, headache, insomnia, mild somnolence, sedation, dry mouth, and sexual dysfunction, but it appears not to lead to much weight gain, and its effects on cognition, cognitive performance are mild. Similar to other antidepressants, the use of sertraline for depression may be associated with a mildly elevated rate of suicidal thoughts in peo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lometraline
Lometraline (International Nonproprietary Name, INN; developmental code name CP-14,368) is a drug and an aminotetralin chemical derivative, derivative. A structural modification of tricyclic compound, tricyclic neuroleptics, lometraline was originally patented by Pfizer as an antipsychotic, tranquilizer, and Management of Parkinson's disease#Medication, antiparkinsonian agent. However, it was instead later studied as a potential antidepressant and/or anxiolytic agent, though clinical studies revealed no psychoactivity at the doses used and further investigation was suspended. Further experimental modifications of the chemical structure of lometraline resulted in the discovery of tametraline, a potency (pharmacology), potent reuptake inhibitor, inhibitor of the reuptake of dopamine and norepinephrine, which in turn led to the discovery of the antidepressant sertraline, a selective serotonin reuptake inhibitor (SSRI). References {{Reflist Dimethylamino compounds Chloroarenes Ps ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pfizer
Pfizer Inc. ( ) is an American Multinational corporation, multinational Pharmaceutical industry, pharmaceutical and biotechnology corporation headquartered at The Spiral (New York City), The Spiral in Manhattan, New York City. Founded in 1849 in New York by German entrepreneurs Charles Pfizer (1824–1906) and Charles F. Erhart (1821–1891), Pfizer is one of the oldest pharmaceutical companies in North America. Pfizer develops and produces medicines and vaccines for immunology, oncology, cardiology, endocrinology, and neurology. The company's largest products by sales are the Pfizer–BioNTech COVID-19 vaccine ($11 billion in 2023 revenues), apixaban ($6 billion in 2023 revenues), a pneumococcal conjugate vaccine ($6 billion in 2023 revenues), palbociclib ($4 billion in 2023 revenues), and tafamidis ($3 billion in 2023 revenues). In 2023, 46% of the company's revenues came from the United States, 6% came from Japan, and 48% came from other countries. Pfizer has been a publi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
1-Aminotetralins
1-Aminotetralin (1-AT), also known as 1-amino-1,2,3,4-tetrahydronaphthalene, is a chemical compound and one of the possible positional isomers of aminotetralin. It consists of a tetralin core with an amino substituent on one of the carbon atoms. Derivatives 1-Aminotetralin is the parent structure of a number of drugs, including the following: Tramazoline is another related compound. See also * 2-Aminotetralin * Aminoindane References External links 1-Aminotetralin - Isomer Design 1-Aminotetralins, {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nefopam
Nefopam, sold under the brand name Acupan among others, is a centrally acting, non-opioid painkilling medication, with central stimulant and sympathomimetic properties that is primarily used to treat moderate to severe pain. History Nefopam is based on a benzoxazocine compound. It was developed in the 1960s and marketed under the name fenazocine. It was initially used in shivering, as a muscle relaxant and as an antidepressant, but then increasingly as an analgesic. Medical uses Analgesic Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial, although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses. The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine with comparable analgesic efficacy to morphine, or oxycodone. Nefopam tends to produce fewer side effects, does not produc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JNJ-7925476
JNJ-7925476 is a triple reuptake inhibitor antidepressant discovered by Johnson & Johnson, but never marketed. These molecules were first prepared by Bruce E. Maryanoff and coworkers during the late 1970s–1980s. The structure is a pyrroloisoquinoline core, with an overlaid benzhydryl motif. Incorporating the pyrrolidine, pyrrolidino ring onto the tetrahydroisoquinoline scaffolding markedly improves potency, although this only works for one of the available stereoisomers. JNJ-7925476 is a racemic preparation of the more potent diastereomer. Of these enantiomers, the eutomer is the (6''R'',10b''S'') stereoisomer, known as JNJ-39836966, and the distomer, (6''S'',10b''R''), is JNJ-39836732 There is some confusion over the nomenclature and Cis–trans isomerism, ''cis''/''trans'' isomeric relationship at the piperidine ring. The compounds as depicted have the carbon of the pyrrolidine carbon and the phenyl ''cis'', but Maryanoff and coworkers are of the opinion that the compound ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EXP-561
EXP-561 is an investigational drug that acts as an inhibitor of the reuptake of serotonin, dopamine, and norepinephrine. It was developed in the 1960s by Du Pont and was suggested as a potential antidepressant Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathi ... but failed in trials and was never marketed. SAR simplification in the molecular structure leads to a compound called 4-Phenylcyclohexylamine 9992-45-1 This is made from 4-phenylcyclohexanone via reduction of the oxime. Such compounds cause a desirable stimulation of the CNS and are antidepressants.Walfred S Saari, US3652769 (1972 to Merck and Co Inc). See also * M.G. 6669 References Amines Experimental antidepressants Serotonin–norepinephrine–dopamine reuptake inhibitors Stimulants Experimental drugs {{ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dasotraline
Dasotraline (INN; former developmental code name SEP-225,289) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) that was under development by Sunovion for the treatment of attention-deficit hyperactivity disorder (ADHD) and binge eating disorder (BED). Structurally, dasotraline is a stereoisomer of desmethylsertraline (DMS), which is an active metabolite of the marketed selective serotonin reuptake inhibitor (SSRI) antidepressant sertraline (Zoloft). Adverse Effects In phase I clinical trials for attention deficit hyperactivity disorder, test subjects reported the following side effects: * Loss of appetite * Dehydration * Dry mouth * Nausea * Insomnia * Anxiety * Panic attacks * Headaches History In 2017, the U.S. Food and Drug Administration accepted Sunovion's New Drug Application (NDA) for review for the treatment of ADHD; however, the NDA was ultimately rejected citing the need for additional studies to determine efficacy and tolerability. In July 2019, S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Desmethylsertraline
Desmethylsertraline (DMS), also known as norsertraline, is an active metabolite of the antidepressant drug sertraline. Like sertraline, desmethylsertraline acts as a monoamine reuptake inhibitor, and may be responsible for some of its parent's therapeutic benefits; however, the effects of DMS's main activity of increasing serotonin levels via binding to the serotonin transporter appears to be negligible as in vivo testing showed no measurable change in brain activity despite a nearly 20-fold increase in DMS blood levels compared to the EC50 (i.e. the amount required to achieve the desired effect in 50% of the population) of its parent drug sertraline. DMS is significantly less potent relative to sertraline as a serotonin reuptake inhibitor (''K''i = 76 nM vs. 3 nM, respectively), but conversely, is more balanced as a monoamine reuptake inhibitor (serotonin, 5-HT (''K''i) = 76 nM; norepinephrine, NE (''K''i) = 420 nM; dopamine, DA (''K''i) = 440 nM), which h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyproheptadine
Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine, first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It was patented in 1959 and came into medical use in 1961. In 2022, it was the 293rd most commonly prescribed medication in the United States, with more than 400,000 prescriptions. Medical uses Cyproheptadine is used to treat allergic reactions (specifically hay fever). There is evidence supporting its use for allergies, but second generation antihistamines such as ketotifen and loratadine have shown equal results with fewer side effects. It is also used as a preventive treatment against migraine. In a 2013 study the frequency of migraine was dramatically reduced in patients within 7 to 10 days after starting treatment. The average frequency of migraine attacks in these patients before administration was 8.7 times per month, this was decreased to 3.1 times per ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
