Cited by 182Treatment of Major DepressionNeurotransmitter Receptor Influence on BehaviorNeuroscience and Neuropharmacology Research

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Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity

Vaishnavi, S.Neil, Nemeroff, Charles B, Plott, Susan J, Rao, Srinivas G, Kranzler, Jay, Owens, Michael J·2004·Biological Psychiatry

DOI 10.1016/j.biopsych.2003.07.006

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Abstract

Background Though selective serotonin reuptake inhibitors have revolutionized the field of psychiatry with demonstrated efficacy in affective and anxiety disorders with minimal side effects, norepinephrine-serotonin reuptake inhibitors may provide efficacy similar to tricyclic antidepressants without the adverse side effects associated with tricyclic antidepressants. Methods The affinity and selectivity of milnacipran, duloxetine, venlafaxine, citalopram, amitriptyline, and nortriptyline were determined for the human serotonin, norepinephrine, and dopamine transporters. Results Both milnacipran and duloxetine were potent inhibitors of serotonin and norepinephrine uptake. Unlike duloxetine and venlafaxine, milnacipran appears serotonin transporter selective in binding (ratio = 2.61) and norepinephrine transporter selective in uptake (ratio =.45). Conclusions Milnacipran's binding and uptake inhibition profile more closely resembles that of the tricyclic antidepressants than that of duloxetine. Whether these differences observed in vitro manifest themselves in vivo is not clear.

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Authors: Vaishnavi, S. N., Nemeroff, C. B., Plott, S. J., Rao, S. G., Kranzler, J., & Owens, M. J.
Affiliations: Emory University (US)
Corresponding author: Owens, Michael J
ORCID: Nemeroff, Charles B
Venue: Biological Psychiatry
Publisher: Elsevier BV
Published: 2004-02
Volume: 55
Issue: 3
Pages: 320-322
ISSN: 0006-3223 (ISSN-L)
DOI: 10.1016/j.biopsych.2003.07.006
OpenAlex: W2113447800
Cited by: 178
References: 15
Citations by year: 2026: 5 · 2025: 4 · 2024: 4 · 2023: 6 · 2022: 7 · 2021: 3 · 2020: 5 · 2019: 5 · 2018: 5 · 2017: 6 · 2016: 5 · 2015: 12 · 2014: 6 · 2013: 13 · 2012: 11
FWCI: 4.60
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Biological Psychiatry (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Pharmacology (medical) › Treatment of Major Depression
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords: milnacipran, serotonin transporter, norepinephrine transporter, dopamine transporter, uptake inhibition, duloxetine, venlafaxine, citalopram, amitriptyline, nortriptyline, tricyclic antidepressants
MeSH terms: Duloxetine Hydrochloride, Venlafaxine Hydrochloride, Milnacipran, Antidepressive Agents, Mental Disorders, Carrier Proteins, Cyclohexanols, Cyclopropanes, Humans, Membrane Glycoproteins, Nerve Tissue Proteins, Neurons, Norepinephrine, Serotonin, Thiophenes, Citalopram, Selective Serotonin Reuptake Inhibitors, Adrenergic Uptake Inhibitors, Membrane Transport Proteins, Symporters, Norepinephrine Plasma Membrane Transport Proteins, Serotonin Plasma Membrane Transport Proteins

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Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity

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