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The pharmacologic selectivity of serotonin reuptake inhibitors

Published online by Cambridge University Press:  16 April 2020

IF Tulloch*
Affiliation:
SmithKline Beecham Pharmaceuticals, Brentford, Middlesex, UK
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Summary

Paroxetine is a highly potent and selective inhibitor of serotonin reuptake, with in vitro potency greater than that of fluoxetine, fluvoxamine, and sertraline. It has little affinity for a wide variety of neurotransmitter receptors, including catecholaminergic or histaminergic systems, in marked contrast to the tricyclic antidepressants. Paroxetine undergoes first-pass metabolism that is partially saturable to give metabolites that are pharmacologically inactive in vivo, unlike those of fluoxetine or sertraline.

Type
Research Article
Copyright
Copyright © Elsevier, Paris 1993

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References

Hall, HOgren, SO (1984) Effects of antidepressant drugs on histamine-H1 receptors in the brain Life Sci 34, 597605CrossRefGoogle Scholar
Johnson, AM (1991) The comparative pharmacological properties of selective serotonin re-uptake inhibitors in animalsIn: Selective Serotonin Reuptake Inhibitors. Perspectives in Psychiatry Vol 1 (Feighner, JP WF Boyer, WF eds). Wiley and Sons, Chichester, 3770Google Scholar
Koe, BK (1990) Preclinical pharmacology of sertraline: a potent and specific inhibitor of serotonin reuptake J Clin Psychiatry 51 (suppl B). 1317Google ScholarPubMed
Nelson, DRPalmer, KJTulloch, IF (1991) Comparative biochemical properties of paroxetine and other selective serotonin re-uptake inhibitors. Presented at ECNP, Monte CarloCrossRefGoogle Scholar
Snyder, SHYamamura, HI (1977) Antidepressants and the muscarinic acetylcholine receptor Arch Gen Psychiatry 34,236239CrossRefGoogle ScholarPubMed
Schmidt, ALebel, LKoe, BKSeger, THeym, J (1989) Sertraline potently displaces (+)-(3H)3-PPP binding to sigma sites in rat brain Eur J Pharmacol 165, 335336CrossRefGoogle ScholarPubMed
Tulloch, IFJohnson, AM (1992) The pharmacologic profile of paroxetine, a new selective serotonin reuptake inhibitor J Clin Psychiatry 53, 2 (suppl), 712Google ScholarPubMed
U'Prichard, DCGreenberg, DASheehan, PBet al (1978) Tricyclic antidepressants: therapeutic properties and affinity for α-noradrenergic receptor binding sites in the brain Science 199, 197198CrossRefGoogle Scholar
Wong, DTThrelkeld, PGRobertson, DW (1991) Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors Neuropsychopharmacology 5, 4347Google ScholarPubMed
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