Biological Activity
Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for α1-, α2- or β-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.
Technical Data
| M. Wt | 445.44 |
| Formula | C19H20FNO3.C4H4O4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 64006-44-6 |
| PubChem ID | 6435921 |
| InChI Key | AEIUZSKXSWGSRU-QXGDPHCHSA-N |
| Smiles | OC(=O)C=C/C(O)=O.FC1=CC=C(C=C1)[C@@H]1CCNC[C@H]1COC1=CC2=C(OCO2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.54 | 100 | |
| ethanol | 44.54 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 445.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.24 mL | 11.22 mL | 22.45 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.49 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
Thomas et al (1987) Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor. Psychopharmacology 93 193 PMID: 2962217
Owens et al (1997) Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites. J.Pharmacol.Exp.Ther. 283 1305 PMID: 9400006
Bourin et al (2001) Paroxetine: a review. CNS Drug Rev. 7 25 PMID: 11420571
Fujishiro et al (2002) Comparison of the anticholinergic effects of the serotonergic antidepressants, paroxetine, fluvoxamine and clomipramine. Eur.J.Pharmacol. 454 183 PMID: 12421645
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