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nomifensine - traduction vers arabe
![0066885}} (1982 to Dso "pharmachim").</ref> Radiolabelled:<ref>Ulin, J.; Gee, A.D.; Malmborg, P.; Tedroff, J.; Långström, B. (1989). "Synthesis of racemic (+) and (−) N-[methyl-11C]nomifensine, a ligand for evaluation of monoamine re-uptake sites by use of positron emission tomography". International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes. 40 (2): 171–176. doi:10.1016/0883-2889(89)90194-9.</ref> Improved method:<ref>Ivanov, T. B.; Mondeshka, Diana M.; Angelova, Ivanka G. (1989). "Verbesserte Synthese von 8-Amino-2-methyl-4-phenyl-1,2,3,4-Tetrahydroisochinolin". Journal für Praktische Chemie. 331 (5): 731–735. doi:10.1002/prac.19893310505.</ref> Overall yield 95%!!:<ref>Venkov, Atanas P.; Vodenicharov, Daniel M. (1990). "A New Synthesis of 1,2,3,4-Tetrahydro-2-methyl-4-phenylisoquinolines". Synthesis. 1990 (03): 253–255. doi:10.1055/s-1990-26846.</ref> Analogs:<ref>Pechulis, Anthony D.; Beck, James P.; Curry, Matt A.; Wolf, Mark A.; Harms, Arthur E.; Xi, Ning; Opalka, Chet; Sweet, Mark P.; Yang, Zhicai; Vellekoop, A. Samuel; Klos, Andrew M.; Crocker, Peter J.; Hassler, Carla; Laws, Mia; Kitchen, Douglas B.; Smith, Mark A.; Olson, Richard E.; Liu, Shuang; Molino, Bruce F. (2012). "4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors". Bioorganic & Medicinal Chemistry Letters. 22 (23): 7219–7222. doi:10.1016/j.bmcl.2012.09.050.</ref> Enantiomers:<ref>Kunstmann, Rudolf; Gerhards, Hermann; Kruse, Hansjoerg; Leven, Margret; Paulus, Erich F.; Schacht, Ulrich; Schmitt, Karl; Witte, Peter U. (1987). "Resolution, absolute stereochemistry, and enantioselective activity of nomifensine and hexahydro-1H-indeno[1,2-b]pyridines". Journal of Medicinal Chemistry. 30 (5): 798–804. doi:10.1021/jm00388a009.</ref>](https://commons.wikimedia.org/wiki/Special:FilePath/Nomifensine synthesis.svg?width=200 "0066885}} (1982 to Dso \"pharmachim\").</ref> Radiolabelled:<ref>Ulin, J.; Gee, A.D.; Malmborg, P.; Tedroff, J.; Långström, B. (1989). \"Synthesis of racemic (+) and (−) N-[methyl-11C]nomifensine, a ligand for evaluation of monoamine re-uptake sites by use of positron emission tomography\". International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes. 40 (2): 171–176. doi:10.1016/0883-2889(89)90194-9.</ref> Improved method:<ref>Ivanov, T. B.; Mondeshka, Diana M.; Angelova, Ivanka G. (1989). \"Verbesserte Synthese von 8-Amino-2-methyl-4-phenyl-1,2,3,4-Tetrahydroisochinolin\". Journal für Praktische Chemie. 331 (5): 731–735. doi:10.1002/prac.19893310505.</ref> Overall yield 95%!!:<ref>Venkov, Atanas P.; Vodenicharov, Daniel M. (1990). \"A New Synthesis of 1,2,3,4-Tetrahydro-2-methyl-4-phenylisoquinolines\". Synthesis. 1990 (03): 253–255. doi:10.1055/s-1990-26846.</ref> Analogs:<ref>Pechulis, Anthony D.; Beck, James P.; Curry, Matt A.; Wolf, Mark A.; Harms, Arthur E.; Xi, Ning; Opalka, Chet; Sweet, Mark P.; Yang, Zhicai; Vellekoop, A. Samuel; Klos, Andrew M.; Crocker, Peter J.; Hassler, Carla; Laws, Mia; Kitchen, Douglas B.; Smith, Mark A.; Olson, Richard E.; Liu, Shuang; Molino, Bruce F. (2012). \"4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors\". Bioorganic & Medicinal Chemistry Letters. 22 (23): 7219–7222. doi:10.1016/j.bmcl.2012.09.050.</ref> Enantiomers:<ref>Kunstmann, Rudolf; Gerhards, Hermann; Kruse, Hansjoerg; Leven, Margret; Paulus, Erich F.; Schacht, Ulrich; Schmitt, Karl; Witte, Peter U. (1987). \"Resolution, absolute stereochemistry, and enantioselective activity of nomifensine and hexahydro-1H-indeno[1,2-b]pyridines\". Journal of Medicinal Chemistry. 30 (5): 798–804. doi:10.1021/jm00388a009.</ref>")
Wikipédia
Nomifensine (Merital, Alival) is a norepinephrine-dopamine reuptake inhibitor, i.e. a drug that increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters. This is a mechanism of action shared by some recreational drugs like cocaine and the medication tametraline (see DRI). Research showed that the (S)-isomer is responsible for activity.
The drug was developed in the 1960s by Hoechst AG (now Sanofi-Aventis), who then test marketed it in the United States. It was an effective antidepressant, without sedative effects. Nomifensine did not interact significantly with alcohol and lacked anticholinergic effects. No withdrawal symptoms were seen after 6 months treatment. The drug was however considered not suitable for agitated patients as it presumably made agitation worse. In January 1986 the drug was withdrawn by its manufacturers for safety reasons.
Some case reports in the 1980s suggested that there was potential for psychological dependence on nomifensine, typically in patients with a history of stimulant addiction, or when the drug was used in very high doses (400–600 mg per day).
In a 1989 study it was investigated for use in treating adult ADHD and proven effective. In a 1977 study it has not proven of benefit in advanced parkinsonism, except for depression associated with the parkinsonism.
