Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity.
Article Details
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Vaishnavi SN, Nemeroff CB, Plott SJ, Rao SG, Kranzler J, Owens MJ
Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity.
Biol Psychiatry. 2004 Feb 1;55(3):320-2.
- PubMed ID
- 14744476 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Amitriptyline Sodium-dependent noradrenaline transporter Protein Humans YesInhibitorDetails Amitriptyline Sodium-dependent serotonin transporter Protein Humans YesInhibitorDetails Duloxetine Sodium-dependent noradrenaline transporter Protein Humans YesInhibitorDetails Duloxetine Sodium-dependent serotonin transporter Protein Humans YesInhibitorDetails Nortriptyline Sodium-dependent noradrenaline transporter Protein Humans YesInhibitorDetails Nortriptyline Sodium-dependent serotonin transporter Protein Humans YesInhibitorDetails Venlafaxine Sodium-dependent noradrenaline transporter Protein Humans YesInhibitorDetails - Binding Properties