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Flesinoksan Reference Vidi još Spoljašnje veze Мени за навигацију„Centrally acting hypotensive agents with affinity for 5-HT1A binding sites inhibit forskolin-stimulated adenylate cyclase activity in calf hippocampus.”185424032079991501303110.1016/S0924-977X(03)00108-1„Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study”857002910.1016/0028-3908(95)00098-Q284216310.1016/0014-2999(88)90651-6135130310.1007/BF02245258„Antianxiety and behavioral suppressant actions of the novel 5-HT1A receptor agonist, flesinoxan”797230110.1016/0091-3057(94)90205-4826331410.1097/00004850-199300830-00005„Pilot study of flesinoxan, a 5-HT1A agonist, in major depression: Effects on sleep REM latency and body temperature.”10.1002/hup.4700804071501303110.1016/S0924-977X(03)00108-1уу

Агонисти серотонинског рецептораПиперазиниБензамидиОрганофлуоридиБензодиоксиниАлкохоли


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Flesinoksan




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elimination_half-life =


Flesinoksan (DU-29,373) je potentan i selektivan parcijalni/skoro-pun agonist 5-HT1A receptora iz fenilpiperazinske klase.[1][2][3]


Flesinoksan je originalno razvijen kao antihipertenziv,[1][2][4] a kasnije je utvrđeno da poseduje antidepresivne i anksiolitske efekte na životinjama.[5][6] Konsekventno, on je klinička ispitivanja su sprovedana za tretman kliničke depresije i generalizovanog anksioznog poremećaja. Utvrđeno je da je ima robastnu efikasnost sa veoma visokom tolerabilnošću,[7][8] ali je zbog nepoznatih razloga njegov razvoj prekinut. Kod pacijenata on poboljšava REM san, snižava telesnu temperaturu, i povišava nivoe ACTH-a, kortizola, prolaktina, i hormona rasta.[8][9]



Reference




  1. ↑ 1,01,1 Schoeffter P, Hoyer D (1988). „Centrally acting hypotensive agents with affinity for 5-HT1A binding sites inhibit forskolin-stimulated adenylate cyclase activity in calf hippocampus.”. Br J Pharmacol. 95 (3): 975—985. PMC 1854240 Слободан приступ. PMID 3207999. 


  2. ↑ 2,02,1 Pitchot W, Wauthy J, Legros JJ, Ansseau M (2004). „Hormonal and temperature responses to flesinoxan in normal volunteers: an antagonist study”. European Neuropsychopharmacology. 14 (2): 151—5. PMID 15013031. doi:10.1016/S0924-977X(03)00108-1. 


  3. ^ Hadrava V, Blier P, Dennis T, Ortemann C, de Montigny C (1995). „Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study”. Neuropharmacology. 34 (10): 1311—26. PMID 8570029. doi:10.1016/0028-3908(95)00098-Q. 


  4. ^ Wouters W, Tulp MT, Bevan P (1988). „Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors”. European Journal of Pharmacology. 149 (3): 213—23. PMID 2842163. doi:10.1016/0014-2999(88)90651-6. 


  5. ^ van Hest A, van Drimmelen M, Olivier B (1992). „Flesinoxan shows antidepressant activity in a DRL 72-s screen”. Psychopharmacology. 107 (4): 474—9. PMID 1351303. doi:10.1007/BF02245258. 


  6. ^ Rodgers RJ, Cole JC, Davies A (1994). „Antianxiety and behavioral suppressant actions of the novel 5-HT1A receptor agonist, flesinoxan”. Pharmacology, Biochemistry, and Behavior. 48 (4): 959—63. PMID 7972301. doi:10.1016/0091-3057(94)90205-4. 


  7. ^ Grof P, Joffe R, Kennedy S, Persad E, Syrotiuk J, Bradford D (1993). „An open study of oral flesinoxan, a 5-HT1A receptor agonist, in treatment-resistant depression”. International Clinical Psychopharmacology. 8 (3): 167—72. PMID 8263314. doi:10.1097/00004850-199300830-00005. 


  8. ↑ 8,08,1 Marc Ansseau; William Pitchot; Antonio Gonzalez Moreno; Jacques Wauthy; Patrick Papart (2004). „Pilot study of flesinoxan, a 5-HT1A agonist, in major depression: Effects on sleep REM latency and body temperature.”. Human Psychopharmacology: Clinical and Experimental. 8 (4): 279—283. doi:10.1002/hup.470080407. [мртва веза]


  9. ^ Pitchot W, Wauthy J, Legros JJ, Ansseau M (2004). „Hormonal and temperature responses to flesinoxan in normal volunteers: an antagonist study”. European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology. 14 (2): 151—5. PMID 15013031. doi:10.1016/S0924-977X(03)00108-1. 



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