Flesinoxan

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Flesinoxan
Systematic (IUPAC) name
4-fluoro-N-(2-{4-[(2S)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-5-yl]piperazin-1-yl}ethyl)benzamide
Clinical data
Pregnancy cat.  ?
Legal status Uncontrolled
Routes Oral
Identifiers
CAS number 98206-10-1
ATC code None
PubChem CID 57347
ChemSpider 51700
UNII 3V574S89E1 YesY
KEGG D02568
Chemical data
Formula C22H26FN3O4 
Mol. mass 415.458 g/mol

Flesinoxan (DU-29,373) is a potent and selective 5-HT1A receptor partial/near-full agonist of the phenylpiperazine class.[1][2][3] Originally developed as an antihypertensive agent,[1][2][4] it was later found to possess antidepressant and anxiolytic effects in animals.[5][6] As a result, it was investigated in human clinical trials for the treatment of major depressive disorder and generalized anxiety disorder and was found to have robust efficacy with very high tolerability,[7][8] but for unclear reasons development was halted and it was never marketed. In patients it enhances REM sleep latency, decreases body temperature, and increases ACTH, cortisol, prolactin, and growth hormone secretion.[8][9]

See also [edit]

References [edit]

  1. ^ a b 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. 
  2. ^ a b 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. 
  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. 
  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. 
  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. 
  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. 
  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. 
  8. ^ a b 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. 
  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. 
GABAA
PAMs
non-N05B
α2δ VDCC Blockers
5-HT1A Agonists
H1 Antagonists
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Others

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc (eval/thrp), drug (N5A/5B/5C/6A/6B/6D)
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