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Tropanserin
Tropanserin ( INN; MDL-72,422) is a drug which acts as a potent and selective 5-HT3 receptor antagonist. It was investigated in clinical trials for the treatment of migraine in the 1980s but was never marketed. Synthesis Tropanserin can be prepared by the reaction of tropine with 3,5-dimethylbenzoyl chloride. See also * Bemesetron * Zatosetron * Ricasetron * Granisetron Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the v ... * Tropisetron References 5-HT3 antagonists Benzoate esters Tropanes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tropanserin Synthesis
Tropanserin (INN; MDL-72,422) is a drug which acts as a potent and selective 5-HT3 receptor antagonist. It was investigated in clinical trials for the treatment of migraine in the 1980s but was never marketed. Synthesis Tropanserin can be prepared by the reaction of tropine with 3,5-dimethylbenzoyl chloride. See also * Bemesetron * Zatosetron * Ricasetron * Granisetron Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the v ... * Tropisetron References 5-HT3 antagonists Benzoate esters Tropanes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tropisetron
Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy, although it has been used experimentally as an analgesic in cases of fibromyalgia. It was patented in 1982 and approved for medical use in 1992. It is on the World Health Organization's List of Essential Medicines. It is marketed by Novartis in Europe, Australia, New Zealand, Japan, South Korea and the Philippines as Navoban, but is not available in the U.S. It is also available from Novell Pharmaceutical Laboratories and marketed in several Asian countries as Setrovel. Pharmacology Tropisetron acts as both a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist. Adverse effects Tropisetron is a well-tolerated drug with few side effects. Headache, constipation, and dizziness are the most commonly reported side effects associated with its use. Hypotension, transient liver enzyme elevation, immune hypersensitivity syndro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ricasetron
Ricasetron (BRL-46470) is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor. It has antiemetic effects as with other 5-HT3 antagonists, and also has anxiolytic effects significantly stronger than other related drugs, and with less side effects than benzodiazepine anxiolytics. However, it has never been developed for medical use. See also * Zatosetron * Bemesetron * Tropanserin *Tropisetron *Granisetron Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the v ... References 5-HT3 antagonists Tropanes Ureas Indoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zatosetron
Zatosetron (LY-277,359) is a drug which acts as an antagonist at the 5HT3 receptor It is orally active and has a long duration of action, producing antinauseant effects but without stimulating the rate of gastrointestinal transport. It is also an effective anxiolytic in both animal studies and human trials, although with some side effects at higher doses. See also * Ondansetron *Bemesetron *Granisetron *Ricasetron *Tropanserin Tropanserin ( INN; MDL-72,422) is a drug which acts as a potent and selective 5-HT3 receptor antagonist. It was investigated in clinical trials for the treatment of migraine in the 1980s but was never marketed. Synthesis Tropanserin can be p ... * Tropisetron References 5-HT3 antagonists Tropanes Salicylamide ethers Chloroarenes Glycine receptor agonists Glycine receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bemesetron
Bemesetron (MDL-72222) is a drug which acts as an antagonist at the 5HT3 receptor. It has antiemetic effects comparable to metoclopramide Metoclopramide is a medication used for stomach and esophageal problems. It is commonly used to treat and prevent nausea and vomiting, to help with emptying of the stomach in people with delayed stomach emptying, and to help with gastroesoph ..., however it is not used clinically, instead its main application is in scientific research studying the involvement of the 5HT3 receptor in the actions of drugs of abuse. See also * Tropanserin * Tropisetron * Zatosetron * Ricasetron * Granisetron References 5-HT3 antagonists Tropanes Benzoate esters Chlorobenzenes Glycine receptor agonists Glycine receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydrochloride
In chemistry, a hydrochloride is an acid salt resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (e.g. an amine). An alternative name is chlorhydrate, which comes from French. An archaic alternative name is muriate, derived from hydrochloric acid's ancient name: muriatic acid. Uses Converting amine In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent su ...s into their hydrochlorides is a common way to improve their water solubility, which can be desirable for substances used in medications. The European Pharmacopoeia lists more than 200 hydrochlorides as active ingredients in medications. These hydrochlorides, compared to free bases, may more readily dissolve in the gastrointestinal tract and be absorbed into the bloodstream more quickly. A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT3 Antagonists
The 5-HT3 antagonists, informally known as "setrons", are a class of drugs that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain. With the notable exceptions of alosetron and cilansetron, which are used in the treatment of irritable bowel syndrome, all 5-HT3 antagonists are antiemetics, used in the prevention and treatment of nausea and vomiting. They are particularly effective in controlling the nausea and vomiting produced by cancer chemotherapy and are considered the gold standard for this purpose. The 5-HT3 antagonists may be identified by the suffix -setron, and are classified under code A04AA of the 's Anatomical Therapeutic Chemical Classification System. Medical uses 5-HT3 antagonists are most effective in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV), especially that caused by highly emetogenic drugs such as cisplatin; whe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Granisetron
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors. Granisetron was developed by chemists working at the British drug company Beecham around 1985 and is available as a generic. It is produced by Roche Laboratories under the trade name Kytril. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA. A granisetron transdermal patch with the trade name Sancuso was approved by the US FDA on September 12, 2008. Sancuso is manufactured by 3M Drug Delivery Systems for Kyowa Kirin, Inc. It was patented in 1985 and approved for medical use in 1991. It is on the World Health O ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tropine
Tropine is a derivative of tropane containing a hydroxyl group at the third carbon. It is also called 3-tropanol. Tropine is a central building block of many chemicals active in the nervous system, including tropane alkaloids. Some of these compounds, such as long-acting muscarinic antagonists are used as medicines because of these effects. Chemistry Synthesis It can be prepared by hydrolysis of atropine. See also * Pseudotropine * Atropine * Tropinone * Tropane alkaloid Tropane alkaloids are a class of bicyclic .2.1alkaloids and secondary metabolites that contain a tropane ring in their chemical structure. Tropane alkaloids occur naturally in many members of the plant family Solanaceae. Certain tropane alkaloid ... References Tropanes Secondary alcohols {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Migraine
Migraine (, ) is a common neurological disorder characterized by recurrent headaches. Typically, the associated headache affects one side of the head, is pulsating in nature, may be moderate to severe in intensity, and could last from a few hours to three days. Non-headache symptoms may include nausea, vomiting, and sensitivity to light, sound, or smell. The pain is generally made worse by physical activity during an attack,as PDF although regular may prevent future attacks. Up to one-third of people affected have |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, pharmaceutical drug, drugs, medical nutrition therapy, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received institutional review board, health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small Pilot experiment, pi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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