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Lidanserin
Lidanserin (INN; ZK-33,839) is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. It was developed as an antihypertensive agent but was never marketed. See also * Glemanserin * Pruvanserin * Roluperidone * Volinanserin * Lenperone * Iloperidone * Ketanserin Ketanserin, sold under the brand name Sufrexal, is an antihypertensive agent which is used to treat arterial hypertension and vasospasm, vasospastic disorders. It is also used in scientific research as an antiserotonergic medication, agent in th ... References 5-HT2A antagonists Abandoned drugs Alpha-1 blockers Antihypertensive agents Ketones 4-Fluorophenyl compounds Piperidines Pyrrolidones {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glemanserin
Glemanserin (INN; developmental code MDL-11,939) is a drug which acts as a potent and selective 5-HT2A receptor antagonist. The first truly selective 5-HT2A ligand to be discovered, glemanserin resulted in the development of the widely used and even more potent and selective 5-HT2A receptor antagonist volinanserin (MDL-100,907), which is a fluorinated analogue. Though it was largely superseded in scientific research by volinanserin, glemanserin was investigated clinically for the treatment of generalized anxiety disorder. However, it was ultimately found to be ineffective and was not marketed. See also * Volinanserin * Pruvanserin * Roluperidone * Lenperone * Lidanserin Lidanserin (INN; ZK-33,839) is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. It was developed as an antihypertensive agent but was never marketed. See also * Glemanserin * Pruvanserin * Roluperidone * Voli ... References 5-HT2A antagonists Secondary alc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lenperone
Lenperone (Elanone-V) is a typical antipsychotic of the butyrophenone chemical class. It was first reported as an anti-emetic in 1974, and its use in treatment of acute schizophrenia was reported in 1975. Related early antipsychotic agents include declenperone and milenperone. Lenperone was never approved by the FDA for use in humans in the United States, but prior to 1989 it was approved for use in veterinary medicine for sedation. Synthesis The alkylation between 2-(3-chloropropyl)-2-(4-fluorophenyl)-1,3-dioxolane [3308-94-9] (1) and 4-(4-fluorobenzoyl)piperidine [56346-57-7] (2) gives 2-(p-fluorophenyl)-2--1,3-dioxolaneCID:20318874(3). Deprotection of the ketal function completes the synthesis of lenperone (4). See also * Glemanserin * Pruvanserin * Roluperidone * Volinanserin Chemically related drugs containing the same 4-(''p''-fluorobenzoyl)piperidine group: * Altanserin * Ketanserin * Setoperone * Lidanserin References Butyrophenone antipsychotics 4-Fl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pruvanserin
Pruvanserin (EMD-281,014, LY-2,422,347) is a selective 5-HT2A receptor antagonist which was under development by Eli Lilly and Company for the treatment of insomnia. It was in phase II clinical trials in 2008 but appears to have been discontinued as it is no longer in the company's development pipeline. In addition to its sleep-improving properties, pruvanserin has also been shown to have antidepressant, anxiolytic, and working memory-enhancing effects in animal studies. See also * Eplivanserin * Pimavanserin * Glemanserin * Roluperidone * Volinanserin * Ziprasidone * Lenperone Lenperone (Elanone-V) is a typical antipsychotic of the butyrophenone chemical class. It was first reported as an anti-emetic in 1974, and its use in treatment of acute schizophrenia was reported in 1975. Related early antipsychotic agents includ ... * Lidanserin References {{Serotonergics 5-HT2A antagonists Drugs developed by Eli Lilly and Company Indoles Aromatic nitriles Piperazi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Roluperidone
Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A receptor, 5-HT2A and sigma-2 receptor, σ2 receptor receptor antagonist, antagonist under development by Minerva Neurosciences for the treatment of schizophrenia. One of its metabolites also has some affinity (pharmacology), affinity for the histamine H1 receptor, H1 receptor. Pre-clinical findings provide evidence of the effect of roluperidone on brain-derived neurotrophic factor ("BDNF"), which has been associated with neurogenesis, neuroplasticity, neuroprotection, synapse regulation, learning and memory. As of May 2018, the drug was in Phases of clinical research#Phase III, phase III clinical trials. In May 2020, the shares of Minerva Neurosciences plummeted 67% after the trial "failed to meet its primary endpoint of reduction in negative symptoms, and key secondary endpoints of improvement in personal and social performance measurements." However, in August 2022 Minerva submitted a New Drug ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Volinanserin
Volinanserin (INN; developmental code MDL-100,907) is a highly selective 5-HT2A receptor antagonist that is frequently used in scientific research to investigate the function of the 5-HT2A receptor. It was also tested in clinical trials as a potential antipsychotic, antidepressant, and treatment for insomnia but was never marketed. Synthesis The synthesis of volinanserin has been reported. Beginning with protection of ethyl isonipecotate (1) with Boc anhydride gives ethyl ''N''-Boc-4-piperidinecarboxylate (2). Ester-amide interchange with ''N''-methoxymethylamine HCl in the presence of carbonyldiimidazole (CDI) coupling agent gives 1-Boc-4- ethoxy(methyl)carbamoyliperidine (3). Weinreb ketone synthesis occurs upon benzoylation with 1,2-dimethoxybenzene (4) to give 1-Boc-4-(3,4-dimethoxybenzoyl)piperidine (5). Acid removal of the urethane protecting group gives (3,4-dimethoxyphenyl)-piperidin-4-ylmethanone (6). The reduction of the ketone with sodium borohydride leads to (3, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Iloperidone
Iloperidone, sold under the brand name Fanapt among others, is an atypical antipsychotic for the treatment of schizophrenia and bipolar I disorder. Medical uses Iloperidone is indicated for the treatment of schizophrenia and mania or mixed affective state, mixed episodes in bipolar I disorder. In a 2013 study in a comparison of 15 antipsychotic drugs in effectivity in treating schizophrenic symptoms, iloperidone demonstrated mild effectiveness — as effective as lurasidone, and 13 to 15% less effective than ziprasidone, chlorpromazine, and asenapine. It generally appears to work better than placebo. Side effects Examination of the safety and tolerability of iloperidone have shown that at a 5 mg/day dose in healthy male volunteers, the drug was fairly well tolerated, although hypotension, dizziness, and somnolence were very common side effects ranging from mild to moderate in severity. A second study showed that co administration of food decreased the severity of these ef ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Antagonists
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and functions as a G protein-coupled receptor (GPCR). It is a cell surface receptor that activates multiple intracellular signalling cascades. Like all 5-HT2 receptors, the 5-HT2A receptor is coupled to the Gq/G11 signaling pathway. It is the primary excitatory receptor subtype among the serotonin-responsive GPCRs. The 5-HT2A receptor was initially noted for its central role as the primary target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. It later regained research prominence when found to mediate, at least in part, the effects of many antipsychotic drugs, particularly atypical antipsychotics. Downregulation of post-synaptic 5-HT2A receptors is an adaptive response triggered by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Elevated 5-HT2A receptor density has been observed in suicidal and ot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketones
In organic chemistry, a ketone is an organic compound with the structure , where R and R' can be a variety of carbon-containing substituents. Ketones contain a carbonyl group (a carbon-oxygen double bond C=O). The simplest ketone is acetone (where R and R' are methyl), with the formula . Many ketones are of great importance in biology and 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 retained IUPAC names, although some introd ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antihypertensive Agents
Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke, heart failure, kidney failure and myocardial infarction. Evidence suggests that a reduction of blood pressure by 5 mmHg can decrease the risk of stroke by 34% and of ischaemic heart disease by 21%. It can reduce the likelihood of dementia, heart failure, and mortality from cardiovascular disease. There are many classes of antihypertensives, which lower blood pressure by different means. Among the most important and most widely used medications are thiazide diuretics, calcium channel blockers, angiotensin-converting enzyme inhibitors (ACE inhibitors), angiotensin II receptor blockers or antagonists (ARBs), and beta blockers. Which type of medication to use initially for hypertension has been the subject of several large studies and resulting national guidelines. The fundamental g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-1 Blockers
Alpha 1 or Alpha-1 may refer to: *Alpha-1 adrenergic receptor, a G protein-coupled receptor *Alpha-1 antitrypsin, a protein **Alpha-1 antitrypsin deficiency Alpha-1 antitrypsin deficiency (A1AD or AATD) is a genetic disorder that may result in lung disease or liver disease. Onset of lung problems is typically between 20 and 50 years of age. This may result in shortness of breath, wheezing, or an inc ..., a genetic disorder * Alpha-1-fetoprotein or Alpha-fetoprotein, a protein *Alpha-One, a fictional spacecraft in '' Buzz Lightyear of Star Command: The Adventure Begins'' * ''Alpha 1'' (Robert Silverberg anthology), a 1970 book * Alpha-1 Wrestling, a professional wrestling promotion See also * * * A1 (other) * Alpha (other) * AMY1A or Alpha-1A or, an enzyme found in humans and other mammals * List of A1 genes, proteins or receptors {{disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The Aba ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
