Flesinoksan
{{Drugbox-lat | IUPAC_name = 4-fluoro-N-(2-{4-[(2S)-2-(hidroksimetil)-2,3-dihidro-1,4-benzodioksin-5-il]piperazin-1-il}etil)benzamid | image = Flesinoxan.svg | width = | image2 = | width2 =
| tradename = | pregnancy_category = | legal_status = Nije kontrolisana supstanca | routes_of_administration = Oralno
| bioavailability = | metabolism = | elimination_half-life = | excretion =
| CAS_number_Ref = 
| CAS_number = 98206-10-1
| ATC_prefix = none
| ATC_suffix =
| PubChem = 57347
| IUPHAR_ligand =
| ChEMBL_Ref =
| ChEMBL =
| DrugBank_Ref =
| DrugBank =
| ChemSpiderID = 51700
| UNII_Ref =
| UNII = 3V574S89E1
| KEGG = D02568
| C=22 | H=26 | F=1 | N=3 | O=4
| molecular_weight = 415,458 g/mol
| smiles = C1CN(CCN1CCNC(=O)C2=CC=C(C=C2)F)C3=C4C(=CC=C3)O[C@H](CO4)CO
| StdInChI_Ref =
| StdInChI =
| StdInChIKey_Ref =
| StdInChIKey =
}}
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
уреди- ^ а б 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
. PMID 3207999.
- ^ а б 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ а б 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. Архивирано из оригинала 17. 12. 2012. г. Приступљено 07. 10. 2012.
- ^ 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.
