Fluparoxan
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| Systematic (IUPAC) name | |
|---|---|
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(3aS,9aS)-5-fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c]pyrrole | |
| Clinical data | |
| Legal status |
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| Routes of administration | Oral |
| Identifiers | |
| CAS Number | 105182-45-4 111793-41-0 (hydrochloride) |
| ATC code | None |
| PubChem | CID 72036 |
| IUPHAR/BPS | 41 |
| ChemSpider | 65029 |
| UNII |
WGA8E072GX  |
| ChEMBL | CHEMBL1765294 |
| Chemical data | |
| Formula | C10H10FNO2 |
| Molar 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.[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 2 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. doi:10.1111/j.1476-5381.1991.tb12272.x. PMC 1917968. PMID 1677298.
- 1 2 Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. 2008. ISBN 0-521-85702-3.
- ↑ 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. doi:10.1111/j.1365-2125.1995.tb04483.x. PMC 1365053. PMID 7669482.
- ↑ 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. doi:10.1111/j.1476-5381.1996.tb15231.x. PMC 1909310. PMID 8821553.
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