|
Centanafadine
Centanafadine (INN) (former developmental code name EB-1020) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) that began its development with Euthymics Bioscience after they acquired DOV Pharmaceutical. It was developed as a treatment for attention-deficit hyperactivity disorder (ADHD) and inhibits the reuptake of norepinephrine Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad' ..., dopamine, and serotonin with a ratio of 1:6:14, respectively. In 2011, Euthymics Bioscience spun off its development of centanafadine to a new company called Neurovance. In March 2017, Otsuka Pharmaceutical acquired Neurovance and the rights to centanafadine. As of January 2018, Otsuka's pipeline indicates it is in Phase III clinical trials. See also * Amitifadine * Bicifadine * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amitifadine
Amitifadine (developmental code names DOV-21,947, EB-1010) is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) or so-called triple reuptake inhibitor (TRI) which is or was being developed by Euthymics Bioscience It was under development for the treatment of major depressive disorder, but in May 2013, it was reported that the drug failed to show superior efficacy to placebo in a phase IIb/ IIIa clinical trial. It was suggested that this may have been due to the drug being underdosed. In September 2017, development of amitifadine for the treatment of major depressive disorder was finally officially discontinued. As of September 2017, it is still listed as being under development for the treatment of alcoholism and smoking withdrawal. Pharmacology Ki values for SERT, NET, and DAT of amitifadine are 99 nM, 262 nM, and 213 nM. The IC50 values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM, respectively Amitifadine reduces the duration o ... [...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 ADHD, 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, Sunovion’s NDA for the treatment o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stimulants
Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have Sympathomimetic drug, sympathomimetic effects. Stimulants are widely used throughout the world as prescription medicines as well as without a prescription (either legally or Prohibition (drugs), illicitly) as performance-enhancing substance, performance-enhancing or recreational drug use, recreational drugs. Among narcotics, stimulants produce a noticeable crash or ''Comedown (drugs), comedown'' at the end of their effects. The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall). It was estimated in 2015 that the percentage of the world population that had used cocaine during a year was 0.4%. For the category "amphetamines and p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tesofensine
Tesofensine (NS2330) is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity. Tesofensine was originally developed by a Danish biotechnology company, NeuroSearch, who transferred the rights to Saniona in 2014. As of 2019, tesofensine has been discontinued for the treatment of Alzheimer's and Parkinson's disease but is in phase III clinical trial for obesity. History Tesofensine was originally investigated for the treatment of Alzheimer's disease and Parkinson's disease, and was subsequently dropped from development for these applications after early trial results showed limited efficacy for treatment of these diseases. However, weight loss was consistently reported as an adverse event in the original studies, especially in overweight or obese patients. Therefore, it was decided to pursue development of tesofensine for the treatment of obesity. Tesofensine primarily acts as an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOV-216,303
DOV 216,303 is an experimental antidepressant drug originally developed by DOV Pharmaceutical and was licensed to Merck & Co. in 2004; Merck and DOV terminated their relationship in December 2006. It is a triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It is the racemic mixture of amitifadine (DOV-21,947) and its (–)- enantiomer, DOV-102,677. Its IC50 values for SERT, NET, and DAT are Ki 14 nM, 20 nM, and 78 nM, respectively. As of March 2008, DOV had no intention to further develop DOV-216,303 because the patent on the compound had expired. In a mouse model, DOV-216,303 has shown the ability to promote recovery after spinal cord contusion A bruise, also known as a contusion, is a type of hematoma of tissue, the most common cause being capillaries damaged by trauma, causing localized bleeding that extravasates into the surrounding interstitial tissues. Most bruises occur clos .... See also * Bicifadine ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bicifadine
Bicifadine (DOV-220,075) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) discovered at American Cyanamid as an analgesic drug candidate, and licensed to DOV Pharmaceutical in 1998 after American Cyanamid was acquired by Wyeth. In January 2007, Dov licensed the rights to bicifadine to XTL Biopharmaceuticals after bicifadine failed in a Phase III clinical trial for chronic lower back pain. XTL ran a PhaseIIb clinical trial for pain caused by diabetic neuropathy, which failed in 2008; XTL terminated the agreement in 2010. In 2010 Dov was acquired by Euthymics Bioscience which intended to continue development of other candidates from Dov's portfolio.Fierce Biotech July 22, 201Euthymics lands $24M to fund antidepressant work/ref> Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs. While the drug is purported to be a seroton ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine
Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic compound, organic chemical of the catecholamine and phenethylamine families. Dopamine constitutes about 80% of the catecholamine content in the brain. It is an amine synthesized by removing a carboxyl group from a molecule of its precursor (chemistry), precursor chemical, L-DOPA, which is biosynthesis, synthesized in the brain and kidneys. Dopamine is also synthesized in plants and most animals. In the brain, dopamine functions as a neurotransmitter—a chemical released by neurons (nerve cells) to send signals to other nerve cells. Neurotransmitters are synthesized in specific regions of the brain, but affect many regions systemically. The brain includes several distinct dopaminergic pathway, dopamine pathways, one of which plays a major role in the motivational component of reward system, reward-motivated behavior. The anticipa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
