Fluparoxan

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Fluparoxan
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • (3aS,9aS)-5-fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]pyrrole
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC10H10FNO2
Molar mass195.19 g/mol g·mol−1
3D model (JSmol)
  • Fc2c1O[C@@H]3[C@@H](Oc1ccc2)CNC3

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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
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