Flesinoksan

Flesinoksan
(IUPAC) ime
	4-fluoro-N-(24-[(2S)-2-(hidroksimetil)-2,3-dihidro-1,4-benzodioksin-5-il]piperazin-1-il
Klinički podaci
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Hemijski podaci
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Pravni status

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 =

| 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 | InChI = | InChIKey = | StdInChI_Ref = | StdInChI = 1S/C22H26FN3O4/c23-17-6-4-16(5-7-17)22(28)24-8-9-25-10-12-26(13-11-25)19-2-1-3-20-21(19)29-15-18(14-27)30-20/h1-7,18,27H,8-15H2,(H,24,28)/t18-/m0/s1 | StdInChIKey_Ref = | StdInChIKey = NYSDRDDQELAVKP-SFHVURJKSA-N }}

Flesinoksan (DU-29,373) je potentan i selektivan parcijalni/skoro-pun agonist 5-HT_1A 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 2 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.
1 2 Pitchot W, Wauthy J, Legros JJ, Ansseau M (March 2004). „Hormonal and temperature responses to flesinoxan in normal volunteers: an antagonist study”. European Neuropsychopharmacology 14 (2): 151–5. DOI:10.1016/S0924-977X(03)00108-1. PMID 15013031.
↑ Hadrava V, Blier P, Dennis T, Ortemann C, de Montigny C (October 1995). „Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study”. Neuropharmacology 34 (10): 1311–26. DOI:10.1016/0028-3908(95)00098-Q. PMID 8570029.
↑ Wouters W, Tulp MT, Bevan P (May 1988). „Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors”. European Journal of Pharmacology 149 (3): 213–23. DOI:10.1016/0014-2999(88)90651-6. PMID 2842163.
↑ van Hest A, van Drimmelen M, Olivier B (1992). „Flesinoxan shows antidepressant activity in a DRL 72-s screen”. Psychopharmacology 107 (4): 474–9. DOI:10.1007/BF02245258. PMID 1351303.
↑ Rodgers RJ, Cole JC, Davies A (August 1994). „Antianxiety and behavioral suppressant actions of the novel 5-HT1A receptor agonist, flesinoxan”. Pharmacology, Biochemistry, and Behavior 48 (4): 959–63. DOI:10.1016/0091-3057(94)90205-4. PMID 7972301.
↑ 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. DOI:10.1097/00004850-199300830-00005. PMID 8263314.
1 2 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. Arhivirano iz originala na datum 2012-12-17. Pristupljeno 2014-04-05.
↑ Pitchot W, Wauthy J, Legros JJ, Ansseau M (March 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. DOI:10.1016/S0924-977X(03)00108-1. PMID 15013031.

Povezano

Vanjske veze

	Portal Medicina
	Portal Hemija

[pmid3207999-1] 1 2 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.

[Pitchot_W,_Wauthy_J,_Legros_JJ,_Ansseau_M_2004_151–5-2] 1 2 Pitchot W, Wauthy J, Legros JJ, Ansseau M (March 2004). „Hormonal and temperature responses to flesinoxan in normal volunteers: an antagonist study”. European Neuropsychopharmacology 14 (2): 151–5. DOI:10.1016/S0924-977X(03)00108-1. PMID 15013031.

[pmid8570029-3] Hadrava V, Blier P, Dennis T, Ortemann C, de Montigny C (October 1995). „Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study”. Neuropharmacology 34 (10): 1311–26. DOI:10.1016/0028-3908(95)00098-Q. PMID 8570029.

[pmid2842163-4] Wouters W, Tulp MT, Bevan P (May 1988). „Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors”. European Journal of Pharmacology 149 (3): 213–23. DOI:10.1016/0014-2999(88)90651-6. PMID 2842163.

[pmid1351303-5] van Hest A, van Drimmelen M, Olivier B (1992). „Flesinoxan shows antidepressant activity in a DRL 72-s screen”. Psychopharmacology 107 (4): 474–9. DOI:10.1007/BF02245258. PMID 1351303.

[pmid7972301-6] Rodgers RJ, Cole JC, Davies A (August 1994). „Antianxiety and behavioral suppressant actions of the novel 5-HT1A receptor agonist, flesinoxan”. Pharmacology, Biochemistry, and Behavior 48 (4): 959–63. DOI:10.1016/0091-3057(94)90205-4. PMID 7972301.

[pmid8263314-7] 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. DOI:10.1097/00004850-199300830-00005. PMID 8263314.

[Marc_Ansseau,_William_Pitchot,_Antonio_Gonzalez_Moreno,_Jacques_Wauthy,_Patrick_Papart_2004_279–283-8] 1 2 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. Arhivirano iz originala na datum 2012-12-17. Pristupljeno 2014-04-05.

[pmid15013031-9] Pitchot W, Wauthy J, Legros JJ, Ansseau M (March 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. DOI:10.1016/S0924-977X(03)00108-1. PMID 15013031.

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