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Paroxetine maleate
Chemical Name:(3S,4R)-3-[(1,3-Benzodioxol-5-yloxy)methyl]-4-(4-fluoro
phenyl)-piperidine maleate
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.
Thomaset al (1987) Biochemical
effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake
inhibitor. Psychopharmacology 93 193. Owenset al
(1997) Neurotransmitter receptor and transporter binding profile of
antidepressants and their metabolites. J.Pharmacol.Exp.Ther. 283
1305. Bourinet al (2001) Paroxetine: a review. CNS Drug Rev. 7
25. Fujishiroet al (2002) Comparison of the anticholinergic
effects of the serotonergic antidepressants, paroxetine, fluvoxamine and
clomipramine. Eur.J.Pharmacol. 454 183.
