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Volinanserin
Volinanserin ( INN) (developmental code name 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. See also * Glemanserin * Pruvanserin * Roluperidone * Lenperone * Lidanserin * Ketanserin * Ritanserin * Eplivanserin * Pimavanserin Pimavanserin (ACP-103; BVF-036), sold under the brand name Nuplazid, is an atypical antipsychotic which is approved for the treatment of Parkinson's disease psychosis and is also being studied for the treatment of Alzheimer’s disease psychos ... References 5-HT2A antagonists Fluoroarenes Piperidines Secondary alcohols Phenol ethers Abandoned drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Roluperidone
Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A and σ2 receptor antagonist under development by Minerva Neurosciences for the treatment of schizophrenia. One of its metabolites also has some affinity for the 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 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 of 2022 Minerva submitted a New Drug Application (NDA) to the Food and Drug Administration (FDA) for the approval of roluperidone for the treatment of schizophrenia. The ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lidanserin
Lidanserin (International Nonproprietary Name, INN; ZK-33,839) is a drug which acts as a combined 5-HT2A receptor, 5-HT2A and α1-adrenergic receptor, α1-adrenergic receptor receptor antagonist, antagonist. It was developed as an antihypertensive agent but was never marketed. See also * Glemanserin * Pruvanserin * Roluperidone * Volinanserin * Lenperone * Iloperidone * Ketanserin References 5-HT2A antagonists Abandoned drugs Alpha-1 blockers Antihypertensive agents Ketones Fluoroarenes Piperidines Pyrrolidones {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and otherwise ... [...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 is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and otherwise ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eplivanserin
Eplivanserin (SR-46,349; planned trade name Ciltyri) was an experimental drug for the treatment of insomnia which was being developed by Sanofi Aventis. Sanofi Aventis announced in December 2009 that it was withdrawing its application for approval of eplivanserin from both the U.S. Food and Drug Administration and the European Medicines Agency. Mechanism of action Eplivanserin is an inverse agonist on the serotonin receptor subtype 5-HT2A. In contrast to older sedating drugs acting on 5-HT2A receptors (e.g., mirtazapine, clozapine, risperidone), eplivanserin has practically no affinity to dopamine, histamine and adrenergic receptors. Study results In a placebo controlled Phase II clinical trial with 351 subjects, eplivanserin reduced the sleep latency by 39 minutes (versus 26 minutes under placebo). Synthesis ] The condensation between 2'-Fluoroacetophenone 45-27-2(5) & 4-hydroxybenzaldehyde 23-08-0(6) give a chalcone intermediate (also an enone), i.eCID:5398292 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glemanserin
Glemanserin (International Nonproprietary Name, INN) (developmental code name MDL-11,939) is a drug which acts as a potency (pharmacology), potent and binding selectivity, selective 5-HT2A receptor, 5-HT2A receptor receptor antagonist, 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 structural analog, analogue. Though it was largely superseded in scientific research by volinanserin, glemanserin was investigated clinical trial, 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 References 5-HT2A antagonists Secondary alcohols Phenol ethers Piperidines {{nervous-system-drug-stub ... [...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 Eli Lilly and Company brands Indoles Aromatic nitriles N-benzoylpiperazines ... [...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 308-94-9(1) and 4-(4-fluorobenzoyl)piperidine 6346-57-7(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 Lidanserin (International Nonproprietary Name, INN; ZK-33,8 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Secondary Alcohols
In chemistry, an alcohol is a type of organic compound that carries at least one hydroxyl () functional group bound to a saturated carbon atom. The term ''alcohol'' originally referred to the primary alcohol ethanol (ethyl alcohol), which is used as a drug and is the main alcohol present in alcoholic drinks. An important class of alcohols, of which methanol and ethanol are the simplest examples, includes all compounds which conform to the general formula . Simple monoalcohols that are the subject of this article include primary (), secondary () and tertiary () alcohols. The suffix ''-ol'' appears in the IUPAC chemical name of all substances where the hydroxyl group is the functional group with the highest priority. When a higher priority group is present in the compound, the prefix ''hydroxy-'' is used in its IUPAC name. The suffix ''-ol'' in non-IUPAC names (such as paracetamol or cholesterol) also typically indicates that the substance is an alcohol. However, some compound ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperidines
Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor described as objectionable, and typical of amines. The name comes from the genus name ''Piper'', which is the Latin word for pepper. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Production Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: : C5H5N + 3 H2 → C5H10NH Pyridine can also be reduce ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pimavanserin
Pimavanserin (ACP-103; BVF-036), sold under the brand name Nuplazid, is an atypical antipsychotic which is approved for the treatment of Parkinson's disease psychosis and is also being studied for the treatment of Alzheimer’s disease psychosis, schizophrenia, agitation, and major depressive disorder. Unlike other antipsychotics, pimavanserin is not a dopamine receptor antagonist. Pharmacology Pharmacodynamics Pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A receptors with high binding affinity ( Ki 0.087 nM) and at serotonin 5-HT2C receptors with lower binding affinity (Ki 0.44 nM). Pimavanserin shows low binding to σ1 receptors (Ki 120 nM) and has no appreciable affinity (Ki >300 nM) to serotonin 5-HT2B, dopamine (including D2), muscarinic acetylcholine, histamine, or adrenergic receptors, or to calcium channels. Pimavanserin has a unique mechanism of action relative to other antipsychotics, behaving as a selective inv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
