|
Pirenperone
Pirenperone (, , ; developmental code names R-47456, R-50656) is a serotonin receptor antagonist described as an antipsychotic and tranquilizer which was never marketed. It is a relatively selective antagonist of the serotonin 5-HT2 receptors and has been used in scientific research to study the serotonin system. In the 1980s, the drug was found to block the effects of the lysergic acid diethylamide (LSD) in animals, and along with ketanserin, led to the elucidation of the 5-HT2A receptor as the biological mediator of the effects of serotonergic psychedelics. Synthesis The sidechain is formed from the cyclization of 2-aminopyridine with 2-Acetylbutyrolactone (2) in PPA gave 3-(2-hydroxyethyl)-2-methylpyrido ,2-ayrimidin-4-one 1078-67-5(3). Halogenation replaces the hydroxy with the chloride leaving group. Many syntheses do both steps in one-pot with phosphorus oxychloride. The 4-(4-Fluorobenzoyl)Piperidine 6346-57-7has 12 known named uses. The alkylation between 3-( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pirenperone Synthesis
Pirenperone (, , ; developmental code names R-47456, R-50656) is a serotonin receptor antagonist described as an antipsychotic and tranquilizer which was never marketed. It is a relatively selective antagonist of the serotonin 5-HT2 receptors and has been used in scientific research to study the serotonin system. In the 1980s, the drug was found to block the effects of the lysergic acid diethylamide (LSD) in animals, and along with ketanserin, led to the elucidation of the 5-HT2A receptor as the biological mediator of the effects of serotonergic psychedelics. Synthesis The sidechain is formed from the cyclization of 2-aminopyridine with 2-Acetylbutyrolactone (2) in PPA gave 3-(2-hydroxyethyl)-2-methylpyrido ,2-ayrimidin-4-one 1078-67-5(3). Halogenation replaces the hydroxy with the chloride leaving group. Many syntheses do both steps in one-pot with phosphorus oxychloride. The 4-(4-Fluorobenzoyl)Piperidine 6346-57-7has 12 known named uses. The alkylation between 3-(2- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ocaperidone
Ocaperidone (R 79598) is a benzisoxazole antipsychotic. It was initially developed by Janssen, later licensed to French laboratory Neuro3D and then acquired in 2007 by German company Evotec. It was found to be more potent than risperidone in animal studies, but its testing was abandoned in 2010 after unfavorable results in human Phase II trials, as while it was effective at controlling symptoms of schizophrenia, ocaperidone produced an unacceptable amount of extrapyramidal side effects.Geerts H, Spiros A, Roberts P, Twyman R, Alphs L, Grace AA. Blinded prospective evaluation of computer-based mechanistic schizophrenia disease model for predicting drug response. ''PLoS One''. 2012;7(12):e49732. Synthesis The last step requires attachment of the sidechain between 3-(2-bromoethyl)-2,9-dimethyl 4H-pyrido ,2-ayrimidin-4-oneCID:18995805(1) and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole 4163-77-9(2) completing the convergent synthesis of Ocaperidone (3).. See also * Benperidol * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Setoperone
Setoperone is a compound that is a ligand to the 5-HT2A receptor. It can be radiolabeled with the radioisotope fluorine-18 and used as a radioligand with positron emission tomography (PET). Several research studies have used the radiolabeled setoperone in neuroimaging for the studying neuropsychiatric disorders, such as depression or schizophrenia. Synthesis The starting material is called 6-(2-hydroxyethyl)-7-methyl-2,3-dihydro- ,3hiazolo,2-ayrimidin-5-oneCID:15586462(1). Halogenation of this with hydrobromic acid in acetic acid giveCID:15586463(2). Sn2 alkylation with 4-(4-fluorobenzoyl)piperidine 6346-57-7(3) under Finkelstein reaction conditions affords setoperone (4). See also * Altanserin * Ketanserin * Pirenperone * Ritanserin Ritanserin, also known by its developmental code name R-55667, is a serotonin antagonist medication described as an anxiolytic, antidepressant, antiparkinsonian agent, and antihypertensive agent. It was never marketed for medical use due to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketanserin
Ketanserin ( INN, USAN, BAN) (brand name Sufrexal; former developmental code name R41468) is a drug used clinically as an antihypertensive agent and in scientific research to study the serotonin system; specifically, the 5-HT2 receptor family. It was discovered at Janssen Pharmaceutica in 1980. It is not available in the United States. Uses Medical uses Ketanserin is classified as an antihypertensive by the World Health Organization and the National Institute of Health. It has been used to reverse pulmonary hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose). The reduction in hypertension is not associated with reflex tachycardia. It has been used in cardiac surgery. A 2000 Cochrane Review found that, compared to placebo, ketanserin did not provide significant relief for people suffering from Raynaud's phenomenon attacks in the setting of progressive systemic sclerosis (an autoimmune disorder). While the frequency of t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketanserin
Ketanserin ( INN, USAN, BAN) (brand name Sufrexal; former developmental code name R41468) is a drug used clinically as an antihypertensive agent and in scientific research to study the serotonin system; specifically, the 5-HT2 receptor family. It was discovered at Janssen Pharmaceutica in 1980. It is not available in the United States. Uses Medical uses Ketanserin is classified as an antihypertensive by the World Health Organization and the National Institute of Health. It has been used to reverse pulmonary hypertension caused by protamine (which in turn was administered to reverse the effects of heparin overdose). The reduction in hypertension is not associated with reflex tachycardia. It has been used in cardiac surgery. A 2000 Cochrane Review found that, compared to placebo, ketanserin did not provide significant relief for people suffering from Raynaud's phenomenon attacks in the setting of progressive systemic sclerosis (an autoimmune disorder). While the frequency of t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Altanserin
Altanserin is a compound that Binding (molecular), binds to the 5-HT2A receptor, 5-HT2A receptor (5-Hydroxytryptamine (serotonin) 2A receptor). Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain, i.e., studies of the 5-HT2A neuroreceptors. Besides human neuroimaging studies altanserin has also been used in the study of rats. An alternative for PET imaging the 5-HT2A receptor is the [Carbon-11, 11C]volinanserin (MDL-100,907) radioligand. 18F-altanserin and tritium, 3H-volinanserin have shown very comparable binding. Both altanserin and MDL 100,907 are 5-HT2A receptor Receptor antagonist, antagonists. [18F]-setoperone can also be used in PET. An alternative SPECT radioligand is the [123I]-5-I-R91150 receptor antagonist. A rapid chemical synthesis of fluorine-18 and deuterium, H-2 dual-labeled altanserin has been described. Other ligands for other parts of the serotonin system used in PET studies are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Antagonist
A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors. Types 5-HT2A antagonists Antagonists of the 5-HT2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). They include, but are not limited to: * Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic. * Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis. * Quetiapine blocks 5-HT2A, 5-HT1A, dopamine receptors D1 and D2, histamine receptor H1, and A1 adrenoreceptors. 5-HT2A/2C antagonists * Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C and Alpha 1 (A1) adrenoreceptors. * Risperidone antipsychotic * Trazodone 5-HT3 antagonists Another subclass consists of drugs selectively acting at the 5-HT3 receptors, and thus are known as 5-HT3 antagonists. They are efficacious i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-(4-Fluorobenzoyl)Piperidine
A coxless four is a rowing boat used in the sport of competitive rowing. It is designed for four persons who propel the boat with sweep oars, without a coxswain. The crew consists of four rowers, each having one oar. There are two rowers on the stroke side (rower's right hand side) and two on the bow side (rower's lefthand side). There is no coxswain, but the rudder is controlled by one of the crew, normally with the rudder cable attached to the toe of one of their shoes which can pivot about the ball of the foot, moving the cable left or right. The steersman may row at bow, who has the best vision when looking over their shoulder, or on straighter courses stroke may steer, since they can point the stern of the boat at some landmark at the start of the course. The equivalent boat when it is steered by a coxswain is called a "coxed four". Racing boats (often called "shells") are long, narrow, and broadly semi-circular in cross-section with gradual tapers, causing little dra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketones
In organic chemistry, a ketone is a functional group with the structure R–C(=O)–R', where R and R' can be a variety of carbon-containing substituents. Ketones contain a carbonyl group –C(=O)– (which contains a carbon-oxygen double bond C=O). The simplest ketone is acetone (where R and R' is methyl), with the formula . Many ketones are of great importance in biology and in industry. Examples include many sugars ( ketoses), many steroids (e.g., testosterone), and the solvent acetone. Nomenclature and etymology The word ''ketone'' is derived from ''Aketon'', an old German word for ''acetone''. According to the rules of IUPAC nomenclature, ketone names are derived by changing the suffix ''-ane'' of the parent alkane to ''-anone''. Typically, the position of the carbonyl group is denoted by a number, but traditional nonsystematic names are still generally used for the most important ketones, for example acetone and benzophenone. These nonsystematic names are considered ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytics
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 a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotics
Antipsychotics, also known as neuroleptics, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. Long-term use can produce adverse effe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
.svg "Click for more on -> 4-(4-Fluorobenzoyl)Piperidine")
