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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 *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 ... 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] |
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 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 ... * Granisetron References 5-HT3 antagonists Tropanes Ureas Indoles {{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, 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 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 ... 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] |
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 ... * 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 syndrom ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antagonist (pharmacology)
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
5-HT3 Receptor
The 5-HT3 receptor belongs to the Cys-loop superfamily of ligand-gated ion channels (LGICs) and therefore differs structurally and functionally from all other 5-HT receptors (5-hydroxytryptamine, or serotonin receptors) which are G protein-coupled receptors. This ion channel is cation-selective and mediates neuronal depolarization and excitation within the central and peripheral nervous systems. As with other ligand gated ion channels, the 5-HT3 receptor consists of five subunits arranged around a central ion conducting pore, which is permeable to sodium (Na), potassium (K), and calcium (Ca) ions. Binding of the neurotransmitter 5-hydroxytryptamine (serotonin) to the 5-HT3 receptor opens the channel, which, in turn, leads to an excitatory response in neurons. The rapidly activating, desensitizing, inward current is predominantly carried by sodium and potassium ions. 5-HT3 receptors have a negligible permeability to anions. They are most closely related by homology to the nicotinic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Transmembrane receptors include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antinauseant
An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer. They may be used for severe cases of gastroenteritis, especially if the patient is dehydrated. Some antiemetics previously thought to cause birth defects appear safe for use by pregnant women in the treatment of morning sickness and the more serious hyperemesis gravidarum. __TOC__ Types * 5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they can be used to treat post-operative and cytotoxic drug nausea & vomiting. However, they can also cause constipation or diarrhea, dry mouth, and fatigue. ** Dolasetron (Anzemet) can be administered in tablet form or in an injection. ** Granisetron (Kytril, Sancuso) can be administered in tablet (Kytril), oral solution (Kytril), injection (K ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ondansetron
Ondansetron, sold under the brand name Zofran among others, is a medication used to prevent nausea and vomiting caused by cancer chemotherapy, radiation therapy, or surgery. It is also effective for treating gastroenteritis. It can be given by mouth or by injection into a muscle or into a vein. Common side effects include diarrhea, constipation, headache, sleepiness, and itchiness. Serious side effects include QT prolongation and severe allergic reaction. It appears to be safe during pregnancy but has not been well studied in this group. It is a serotonin 5-HT3 receptor antagonist. It does not have any effect on dopamine receptors or muscarinic receptors. Ondansetron was patented in 1984 and approved for medical use in 1990. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication. In 2020, it was the 83rd most commonly prescribed medication in the United States, with more than 8million prescriptions. Medical uses A ... [...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 ... [...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; when used ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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