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Fluparoxan

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Fluparoxan
File:Fluparoxan.png
Systematic (IUPAC) name
(3aS,9aS)-5-fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]pyrrole
Clinical data
  • Uncontrolled
Oral
Identifiers
105182-45-4 111793-41-0 (hydrochloride)
None
PubChem CID 72036
ChemSpider 65029
UNII WGA8E072GX 7pxY
ChEMBL CHEMBL1765294
Chemical data
Formula C10H10FNO2
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.[1][2] 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.[1][2][3][4]

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. doi:10.1111/j.1476-5381.1991.tb12272.x. 
  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. doi:10.1111/j.1365-2125.1995.tb04483.x. 
  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. doi:10.1111/j.1476-5381.1996.tb15231.x.