Fluparoxan

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Fluparoxan
Systematic (IUPAC) name
(3aS,9aS)-5-fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]pyrrole
Clinical data
Pregnancy cat.  ?
Legal status Uncontrolled
Routes Oral
Identifiers
CAS number 105182-45-4 111793-41-0 (hydrochloride)
ATC code None
PubChem CID 72036
ChemSpider 65029
UNII WGA8E072GX YesY
ChEMBL CHEMBL1765294
Chemical data
Formula C10H10FNO2 
Mol. mass 195.19 g/mol

Fluparoxan (GR-50,360) is a potent and highly selective α2-adrenergic receptor antagonist which was being investigated as an antidepressant but failed to show sufficiently significant efficacy for depression in clinical trials and never made it to the market.12 In animal and/or human studies fluparoxan has been found to produce stimulation, tachycardia, hypertension, hyperthermia, penile erection, and pro-nociceptive effects, as well as antidepressant-like effects, panic, and anxiogenesis.1234

See also

References

  1. ^ a b Halliday CA, Jones BJ, Skingle M, Walsh DM, Wise H, Tyers MB (April 1991). "The pharmacology of fluparoxan: a selective alpha 2-adrenoceptor antagonist". British Journal of Pharmacology 102 (4): 887–95. PMC 1917968. PMID 1677298. 
  2. ^ a b Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. 2008. ISBN 0-521-85702-3. 
  3. ^ Johnson MA, Blackwell CP, Smith J (May 1995). "Antagonism of the effects of clonidine by the alpha 2-adrenoceptor antagonist, fluparoxan". British Journal of Clinical Pharmacology 39 (5): 477–83. PMC 1365053. PMID 7669482. 
  4. ^ Vayssettes-Courchay C, Bouysset F, Cordi AA, Laubie M, Verbeuren TJ (February 1996). "A comparative study of the reversal by different alpha 2-adrenoceptor antagonists of the central sympatho-inhibitory effect of clonidine". British Journal of Pharmacology 117 (3): 587–593. PMC 1909310. PMID 8821553.