Paroxetine maleate

Biological Activity

Paroxetine maleate is a highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (K_i = 0.05 nM). K_i 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-HT_2A, 5-HT_1A, D₂ or H₁ receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (K_i = 42 nM). Antidepressant and anxiolytic in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor.
   Thomas et al.
   Psychopharmacology, 1987;93:193
2. Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.
   Owens et al.
   J.Pharmacol.Exp.Ther., 1997;283:1305
3. Paroxetine: a review.
   Bourin et al.
   CNS Drug Rev., 2001;7:25
4. Comparison of the anticholin. effects of the serotonergic antidepressants, paroxetine, fluvox. and clomipramine.
   Fujishiro et al.
   Eur.J.Pharmacol., 2002;454:183

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