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

S. Neil Vaishnavi, Charles Nemeroff, Susan J. Plott, Srinivas G. Rao, Jay Kranzler, Michael J. Owens

Research output: Contribution to journalArticle

125 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)320-322
Number of pages3
JournalBiological Psychiatry
Volume55
Issue number3
DOIs
StatePublished - Feb 1 2004
Externally publishedYes

Fingerprint

Tricyclic Antidepressive Agents
Norepinephrine Plasma Membrane Transport Proteins
Serotonin Plasma Membrane Transport Proteins
Nortriptyline
Citalopram
Dopamine Plasma Membrane Transport Proteins
Amitriptyline
Serotonin Uptake Inhibitors
Anxiety Disorders
Mood Disorders
Psychiatry
Duloxetine Hydrochloride
milnacipran
Venlafaxine Hydrochloride
Serotonin and Noradrenaline Reuptake Inhibitors

Keywords

  • Human dopamine transporter
  • Human norepinephrine transporter
  • Human serotonin transporter
  • Milnacipran
  • Monoamine uptake
  • Transporter binding

ASJC Scopus subject areas

  • Biological Psychiatry

Cite this

Milnacipran : A comparative analysis of human monoamine uptake and transporter binding affinity. / Vaishnavi, S. Neil; Nemeroff, Charles; Plott, Susan J.; Rao, Srinivas G.; Kranzler, Jay; Owens, Michael J.

In: Biological Psychiatry, Vol. 55, No. 3, 01.02.2004, p. 320-322.

Research output: Contribution to journalArticle

Vaishnavi, S. Neil ; Nemeroff, Charles ; Plott, Susan J. ; Rao, Srinivas G. ; Kranzler, Jay ; Owens, Michael J. / Milnacipran : A comparative analysis of human monoamine uptake and transporter binding affinity. In: Biological Psychiatry. 2004 ; Vol. 55, No. 3. pp. 320-322.
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