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 language | English |
|---|---|
| Pages (from-to) | 320-322 |
| Number of pages | 3 |
| Journal | Biological Psychiatry |
| Volume | 55 |
| Issue number | 3 |
| DOIs | |
| State | Published - Feb 1 2004 |
| Externally published | Yes |
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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 journal › Article
}
TY - JOUR
T1 - Milnacipran
T2 - A comparative analysis of human monoamine uptake and transporter binding affinity
AU - Vaishnavi, S. Neil
AU - Nemeroff, Charles
AU - Plott, Susan J.
AU - Rao, Srinivas G.
AU - Kranzler, Jay
AU - Owens, Michael J.
PY - 2004/2/1
Y1 - 2004/2/1
N2 - 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.
AB - 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.
KW - Human dopamine transporter
KW - Human norepinephrine transporter
KW - Human serotonin transporter
KW - Milnacipran
KW - Monoamine uptake
KW - Transporter binding
UR - http://www.scopus.com/inward/record.url?scp=1642441739&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=1642441739&partnerID=8YFLogxK
U2 - 10.1016/j.biopsych.2003.07.006
DO - 10.1016/j.biopsych.2003.07.006
M3 - Article
C2 - 14744476
AN - SCOPUS:1642441739
VL - 55
SP - 320
EP - 322
JO - Biological Psychiatry
JF - Biological Psychiatry
SN - 0006-3223
IS - 3
ER -