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Itameline
Itameline (; developmental code name RU-47213) is a non-selective muscarinic acetylcholine receptor agonist which was under development for the treatment of Alzheimer's disease and memory disorders but was never marketed. It has been referred to as a "nootropic" (cognitive enhancer). The drug is a prodrug of RU-35963, an arecoline derivative. It is an agonist of the muscarinic acetylcholine M1 receptor as well as of other muscarinic acetylcholine receptors. Itameline is described as being superior to arecoline in terms of potency, central selectivity, and duration of action. The drug shows antiamnesic effects in animals, for instance reversing scopolamine-induced memory deficits. Structurally, it is a tetrahydropyridine similarly to xanomeline and milameline. Itameline was first described in the scientific literature by 1992. It was under development by Hoechst Marion Roussel and reached phase 2 clinical trial Clinical trials are prospective biomedical or behavioral re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
M1 Receptor
The muscarinic acetylcholine receptor M1, also known as the cholinergic receptor, muscarinic 1, is a muscarinic receptor that in humans is encoded by the ''CHRM1'' gene. It is localized to 11q13. This receptor is found mediating slow EPSP at the ganglion in the postganglionic nerve, is common in exocrine glands and in the CNS. It is predominantly found bound to G proteins of class Gq that use upregulation of phospholipase C and, therefore, inositol trisphosphate and intracellular calcium as a signalling pathway. A receptor so bound would not be susceptible to CTX or PTX. However, Gi (causing a downstream decrease in cAMP) and Gs (causing an increase in cAMP) have also been shown to be involved in interactions in certain tissues, and so would be susceptible to PTX and CTX respectively. Effects * EPSP in autonomic ganglia * Secretion from salivary glands * Gastric acid secretion from stomach * Via the central nervous system (especially within the brain); mediating certain ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
In chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants and .The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. \begin \ce;& \quad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiamnesic
Nootropics ( or ) (colloquially brain supplements, smart drugs, cognitive enhancers, memory enhancers, or brain boosters) are chemical substances which purportedly improve cognitive functions, such as attention, memory, wakefulness, and self-control. In the United States, nootropics can be over-the-counter drugs and commonly advertised with unproven claims of effectiveness for improving cognition. The Federal Trade Commission and FDA have warned manufacturers and consumers about possible advertising fraud and marketing scams concerning nootropic supplements. Nootropics include both prescription drugs and dietary supplements marketed to enhance brain function, but while FDA-approved drugs have proven benefits and oversight, many dietary supplements lack evidence, may contain unapproved or hidden drugs, and pose safety and regulatory risks.Nootropics: Drugs vs Dietary Supplements for Brain Health. Operation Supplement Safety. https://www.opss.org/article/nootropics-drugs-vs-di ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenol Esters
Phenol (also known as carbolic acid, phenolic acid, or benzenol) is an aromatic organic compound with the molecular formula . It is a white crystalline solid that is volatile and can catch fire. The molecule consists of a phenyl group () bonded to a hydroxy group (). Mildly acidic, it requires careful handling because it can cause chemical burns. It is acutely toxic and is considered a health hazard. Phenol was first extracted from coal tar, but today is produced on a large scale (about 7 million tonnes a year) from petroleum-derived feedstocks. It is an important industrial commodity as a precursor to many materials and useful compounds, and is a liquid when manufactured. It is primarily used to synthesize plastics and related materials. Phenol and its chemical derivatives are essential for production of polycarbonates, epoxies, explosives such as picric acid, Bakelite, nylon, detergents, herbicides such as phenoxy herbicides, and numerous pharmaceutical drugs. Propertie ... [...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] |
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] |
Phases Of Clinical Research
The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases start with testing for drug safety in a few human subjects, then expand to many study participants (potentially tens of thousands) to determine if the treatment is effective. Clinical research is conducted on drug candidates, vaccine candidates, new medical devices, and new diagnostic assays. Description Clinical trials testing potential medical products are commonly classified into four phases. The drug development process will normally proceed through all four phases over many years. When expressed specifically, a clinical trial phase is capitalized both in name and Roman numeral, such as "Phase I" clinical trial. If the drug successfully passes through Phases I, II, and III, it will usually be approved by the national regulatory aut ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hoechst Marion Roussel
Hoechst AG () was a German chemicals, later life sciences, company that became Aventis Deutschland after its merger with France's Rhône-Poulenc S.A. in 1999. With the new company's 2004 merger with Sanofi-Synthélabo, it became a subsidiary of the resulting Sanofi-Aventis pharmaceuticals group. History The company was founded in 1863 as "Teerfarbenfabrik Meister, Lucius & Co." in Höchst, near Frankfurt and changed its name some years later to "Teerfarbenfabrik Meister Lucius & Brüning". In 1880, it became a stock company "Farbwerke vorm. Meister Lucius & Brüning AG". For the international market the name was simplified to "Farbwerke Hoechst AG". Until 1925, the Hoechst AG was independent. In 1916, the Hoechst AG was one of the co-founders of IG Farben, an advocacy group of Germany's chemicals industry to gain industrial power during and after World War I. In 1925, IG Farben turned from an advocacy group into the well-known conglomerate. World War II Various Hoechst fa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Scientific Literature
Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical contributions. These papers serve as essential sources of knowledge and are commonly referred to simply as "the literature" within specific research fields. The process of academic publishing involves disseminating research findings to a wider audience. Researchers submit their work to reputable journals or conferences, where it undergoes rigorous evaluation by experts in the field. This evaluation, known as peer review, ensures the quality, validity, and reliability of the research before it becomes part of the scientific literature. Peer-reviewed publications contribute significantly to advancing our understanding of the world and shaping future research endeavors. Original scientific research first published in scientific journals co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Milameline
Milameline (CI-979, PD-129,409, RU-35,926) is a non-selective muscarinic acetylcholine receptor partial agonist with cognition-acting properties that was being investigated for the treatment of Alzheimer's disease, but produced poor results in clinical trials and was subsequently discontinued. *Changing the ''O''-methyl aldoxime to an ''O''-propargyl oxime instead gives a separate molecule called RU 35986. See also * Alvameline * Sabcomeline * Tazomeline * Xanomeline Xanomeline (developmental code name LY-246,708) is a small molecule muscarinic acetylcholine receptor agonist that was synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the tre ... References {{Muscarinic acetylcholine receptor modulators Abandoned drugs Aldoximes M1 receptor agonists M2 receptor agonists M3 receptor agonists M4 receptor agonists M5 receptor agonists Oxime ethers Tetrahydropyridines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Xanomeline
Xanomeline (developmental code name LY-246,708) is a small molecule muscarinic acetylcholine receptor agonist that was synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the treatment of central nervous system (CNS) disorders. Its pharmacological action is mediated primarily through stimulation of central nervous system muscarinic M1 and M4 receptor subtypes. Xanomeline is a non-selective muscarinic acetylcholine receptor agonist with similar high affinity for all five muscarinic acetylcholine receptor subtypes but has greater agonistic activity at the M1 and M4 subtypes. Xanomeline/trospium (Cobenfy), is a combination medication used in the treatment of schizophrenia. Pharmacology Pharmacodynamics Muscarinic acetylcholine receptor agonist Xanomeline is an agonist that primarily targets the muscarinic acetylcholine receptor family of five muscarinic receptor subtypes, which are designated M1-M5. Whi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
