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Restrict the search for
fluoxetine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
S-fluoxetine is an enantiomer of fluoxetine, a potent and selective inhibitor of the neuronal serotonin-uptake carrier and a clinically effective antidepressant. R-fluoxetine and S-fluoxetine enantiomers are nearly equipotent at blocking serotonin reuptake. In all biochemical and pharmacological studies, the eudismic ratio for the fluoxetine enantiomers is also near unity. A study examining the relative contributions of CYP enzymes to the metabolism of S-fluoxetine, and R-fluoxetine found dramatic differences. These data led to discovery programs between Lilly and Sepracor for the individual enantiomers. S-fluoxetine was studied in a phase 2 clinical trial for the prophylaxis of migraine, however, development was discontinued.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Norfluoxetine is an active N-desmethyl metabolite of the antidepressant fluoxetine that inhibits serotonin uptake. Norfluoxetine is selective serotonin reuptake inhibitor (SSRI) but little is known about its pharmacological actions. Seproxetine (S- Norfluoxetine) was being investigated by Eli Lilly as an antidepressant but development was never completed and the drug was never marketed.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
LY94939 was discovered as a result of efforts to develop agents that inhibit the uptake of 5-HT from the synaptic cleft. A selected analogue of LY94939, the
compound LY82816 (3-p-trifluoromethyl-phenoxyN-methyl-3-phenylpropylamine oxalate or (fluoxetine oxalate), which was a secondary amine (later named as fluoxetine oxalate), and its primary amine or N-demethylated compound
(later named as norfluoxetine), were the most potent inhibitors of [3
H]-5-HT uptake in nerve endings, with Ki values of 0.07 uM. The first salt
form of fluoxetine tested in serotonin reuptake assays in the
early 1970s was the oxalate salt (LY82816); however, the
marketed version is the hydrochloride salt (fluoxetine hydrochloride
(LY110140), or Prozac.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
The selective serotonin reuptake inhibitor fluoxetine consists of equal amounts of R and S stereoisomers (antidepressant Prozac (racemic fluoxetine). Binding to the transporter confirmed selectivity of R- and S-fluoxetine for the 5-HT transporter versus the dopamine (DA) and norepinephrine (NE) human transporters. In addition, receptor binding studies demonstrated significant affinity of R-fluoxetine, but not S-fluoxetine, for human 5-HT(2A) and 5-HT(2C) receptor subtypes. R-fluoxetine acts as an antagonist at 5-HT(2A) and 5-HT(2C) receptors. The attempt to develop a single-enantiomer formulation of fluoxetine for the treatment of depression was unsuccessful. Eli Lilly has terminated its licensing and development agreement with Marlborough, Mass.-based Sepracor for (R)-fluoxetine, the single-isomer version of Lilly's antidepressant Prozac.R-enantiomer of fluoxetine, at its highest administered dose, led to statistically significant prolongation of cardiac repolarization in phase II studies; the studies were subsequently stopped.
Status:
Investigational
Source:
NCT03534063: Not Applicable Interventional Completed Pain, Postoperative
(2018)
Source URL:
Class:
PROTEIN
Status:
Possibly Marketed Outside US
Source:
NCT04619927: Phase 4 Interventional Recruiting Peripheral Arterial Disease
(2021)
Source URL:
Class:
PROTEIN
Status:
Possibly Marketed Outside US
Source:
NCT02710747: Phase 4 Interventional Unknown status Heart Valve Disease
(2015)
Source URL:
Class:
PROTEIN
