Details
Stereochemistry | RACEMIC |
Molecular Formula | C18H20N2.ClH |
Molecular Weight | 300.826 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1CCN2C(C1)C3=C(CC4=C2C=CC=C4)C=CC=C3
InChI
InChIKey=YNPFMWCWRVTGKJ-UHFFFAOYSA-N
InChI=1S/C18H20N2.ClH/c1-19-10-11-20-17-9-5-3-7-15(17)12-14-6-2-4-8-16(14)18(20)13-19;/h2-9,18H,10-13H2,1H3;1H
DescriptionSources: https://www.drugbank.ca/drugs/DB06148Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/15771415 | http://www.medicines.org.au/files/mkptolvo.pdf
Sources: https://www.drugbank.ca/drugs/DB06148
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/15771415 | http://www.medicines.org.au/files/mkptolvo.pdf
Mianserin is a tetracyclic antidepressant used for the treatment of depression. It was investigated as an adjuvant for reduction of negative and cognitive symptoms of schizophrenia, as an aid for opioid detoxification therapy (where it reduced symptoms but lead to higher drop-out rate), and for the treatment of post-traumatic stress disorder (where it was ineffective). Mianserin has a broad spectrum of activity with the most potent binding to 5-HT2A, 5-HT2C, H1, alpha2A and alpha2C receptor.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771415 |
4.3 nM [Ki] | ||
Target ID: CHEMBL225 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771415 |
4.4 nM [Ki] | ||
Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771415 |
1.7 nM [Ki] | ||
Target ID: CHEMBL1867 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771415 |
4.8 nM [Ki] | ||
Target ID: CHEMBL1916 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771415 |
3.8 nM [Ki] | ||
Target ID: CHEMBL304 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771415 |
101.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | TOVLON Approved UseFor the treatment of major depression. |
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Palliative | Unknown Approved UseUnknown |
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Palliative | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. | 1999 Jul |
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High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action. | 1999 May |
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Pharmacology of rapid-onset antidepressant treatment strategies. | 2001 |
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Mirtazapine versus venlafaxine in hospitalized severely depressed patients with melancholic features. | 2001 Aug |
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m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT(2C) receptors but not 5-HT(2A) or 5-HT(2B) receptors. | 2001 Dec |
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Comment: serotonin syndrome induced by fluvoxamine and mirtazapine. | 2001 Dec |
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First report of mirtazapine-induced arthralgia. | 2001 Dec |
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Inhibition of stress- or anxiogenic-drug-induced increases in dopamine release in the rat prefrontal cortex by long-term treatment with antidepressant drugs. | 2001 Feb |
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Treatment of depression in the elderly. | 2001 Feb 1 |
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Serotonergic mechanism in imipramine induced antinociception in rat tail flick test. | 2001 Jan |
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[Comparative study of paroxetine and mianserin in depression in elderly patients: efficacy, tolerance, serotonin dependence]. | 2001 Jan-Feb |
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[Postoperative pain syndrome and its relationship with individual psychological features of personality]. | 2001 Jul-Aug |
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Efficacy and safety of mirtazapine in major depressive disorder patients after SSRI treatment failure: an open-label trial. | 2001 Jun |
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Transcranial magnetic stimulation and antidepressive drugs share similar cellular effects in rat hippocampus. | 2001 Jun |
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Discovery of a novel member of the histamine receptor family. | 2001 Mar |
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Mitrazapine-associated palinopsia. | 2001 May |
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[Interference in the serotoninergic and noradrenergic system. Faster out of depression]. | 2001 Nov 1 |
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Trait anxiety and the effect of a single high dose of diazepam in unipolar depression. | 2001 Nov-Dec |
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Efficacy of mirtazapine for prevention of depressive relapse: a placebo-controlled double-blind trial of recently remitted high-risk patients. | 2001 Oct |
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Fluvoxamine augmentation increases serum mirtazapine concentrations three- to fourfold. | 2001 Oct |
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Prevention of the stress-induced increase in frontal cortical dopamine efflux of freely moving rats by long-term treatment with antidepressant drugs. | 2001 Oct |
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Treatment of mood-congruent psychotic depression with imipramine. | 2001 Oct |
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Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor. | 2001 Oct |
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Mirtazapine for treatment of depression and comorbidities in Alzheimer disease. | 2001 Sep |
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Mania associated with mirtazapine augmentation of fluoxetine. | 2002 |
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Mirtazapine overdose with benign outcome. | 2002 Apr |
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Imipramine, mianserine and maprotiline block delayed rectifier potassium current in ventricular myocytes. | 2002 Feb |
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A double-blind, placebo-controlled study of antidepressant augmentation with mirtazapine. | 2002 Jan 15 |
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Heart rate variability as predictor of nonresponse to mirtazapine in panic disorder: a preliminary study. | 2002 Mar |
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Antidepressant treatments induce the expression of basic fibroblast growth factor in cortical and hippocampal neurons. | 2002 May |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.medicines.org.au/files/mkptolvo.pdf
The initial dosage of Tolvon should be judged individually. It is recommended that treatment begins with a daily dose of 30mg given in three divided doses or a single bedtime dose and be adjusted weekly in the light of the clinical response. The effective daily dose for adult patients usually lies between 30mg and 90mg (average 60mg) in divided doses or as a single bedtime dose. A maximum daily dose of 120mg should not be exceeded.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15771415
Binding of mianserin to 5-HT2A receptor was measured using radioligand binding assay, using [125I]R91150 as a radioligand, and cloned human receptors. pKi for displacement of R91150 was 4.3 nM.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C72900
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NCI_THESAURUS |
C66885
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NCI_THESAURUS |
C265
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244-426-7
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SUB03283MIG
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DBSALT000957
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203127
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100000090114
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21535-47-7
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759590
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31843
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C87210
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CHEMBL6437
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m7521
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2X03TN217S
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68551
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DTXSID30944145
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ACTIVE MOIETY
SUBSTANCE RECORD