A Comparison of the Physicochemical and Biological Properties of Mirtazapine and Mianserin

  title={A Comparison of the Physicochemical and Biological Properties of Mirtazapine and Mianserin},
  author={Jan Kelder and Carel W. Funke and Thus Boer and Leon P. C. Delbressine and Dirk D. Leysen and Victor Johannes Nickolson},
  journal={Journal of Pharmacy and Pharmacology},
Although the chemical structures of the antidepressants mirtazapine and mianserin are closely related there are considerable differences in their biological properties. To find an explanation of this, various physicochemical properties of mirtazapine and mianserin were measured or calculated. 

Antitumor activity of mianserin (a tetracyclic antidepressant) primarily driven by the inhibition of SLC1A5-mediated glutamine transport

The current findings confirmed the feasibility of targeting SLC1A5-mediated glutamine uptake as a novel approach for antitumor intervention and it is anticipated that structural insights obtained based on homology modeling would lead to the discovery of more potent and specific SLC 1A5 inhibitors for clinical development.

Metabolism of the antidepressant mirtazapine in vitro: contribution of cytochromes P-450 1A2, 2D6, and 3A4.

Induction/inhibition or genetic polymorphisms of CYP2D6, CYP1A2, and CYP3A4 may affect MIR metabolism, but involvement of several enzymes in different metabolic pathways may prevent large alterations in in vivo drug clearance.

In vitro metabolism of mirtazapine enantiomers by human cytochrome P450 enzymes

The metabolism of mirtazapine enantiomers was investigated in vitro using human lymphoblast microsomes transfected with human cDNA to overexpress either CYP1A2, CYP2C9, CYP2C19, CYP2D6 or CYP3A4 and

Enantioseparation and molecular modeling study of eight psychoactive drugs on a coated polysaccharide‐based chiral stationary phase

Chiral separation mechanisms have been discussed in detail, and it has been confirmed that hydrogen bond, π–π, hydrophobic interactions, and some special interactions synergistically contributed to the enantioseparation of psychoactive drugs.

Enantiomeric separation of mirtazapine and its metabolites by nano-liquid chromatography with UV-absorption and mass spectrometric detection.

The nanoLC system was connected to a mass spectrometer through a nanoelectrospray interface and the MS, MS2, and MS3 spectra were acquired showing the potential of the system used for characterization and identification of the separated analytes.



Elucidation of the structural requirements for the bioactivation of mianserin in‐vitro

The data are consistent with the proposal that one or more iminium ions derived from mianserin are responsible for the cytotoxicity observed in this in‐vitro system and that appropriate chemical modification may preclude bioactivation of mianserserin by P450 enzymes.

Possible role of free radical formation in clozapine (clozaril)-induced agranulocytosis.

It can be concluded from these data that radical scavengers such as ascorbic acid, when coadministered with clozapine to patients, may reduce oxidative stress and protein adduct formation.

Biotransformation of mianserin in laboratory animals and man.

The biotransformation and excretion of the antidepressant mianserin were studied after oral administration of the labelled drug to rats, mice, rabbits, guinea pigs and humans and a quaternary N-glucuronide was found only in man.

The metabolism of mianserin in women, rabbits, and rats: identification of the major urinary metabolites.

The biotransformation of orally administered 3H-mianserin was investigated in female human subjects, rabbits, and rats by identification of the major urinary metabolites and novel N-formyl compounds were detected in the urine of both animal species.

Citalopram — Pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity

  • J. Hyttel
  • Chemistry, Psychology
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1982

Bioavailability of mirtazapine from Remeron® tablets after single and multiple oral dosing

The absolute bioavailability of mirtazapine, the active constituent of Remeron® tablets, a new antidepressant developed under the laboratory code Org 3770, was assessed in eight healthy young male volunteers after a single oral dose and during multiple oral dosing for seven days, which was not significantly different from the bioavailability at steady state.

Metabolism of three pharmacologically active drugs in isolated human and rat hepatocytes: analysis of interspecies variability and comparison with metabolism in vivo.

The reflection of interspecies differences in isolated hepatocytes, with respect to both metabolite profiles and human-specific metabolites, renders isolated human hepatocytes a very valuable tool during preclinical drug development.

Possible Role of Free Radical Formation in Drug-Induced Agranulocytosis

Ascorbate, when coadministered with agranulocytosis-causing drugs, may inhibit free radical chain reactions and other free radical-mediated reactions, such as protein adduct formation, and thereby prevent drug-induced agranutosis.