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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
Structure of Mianserin Hydrochloride

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

HIDE SMILES / InChI

Molecular Formula C18H20N2
Molecular Weight 264.3648
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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 TargetPharmacologyConditionPotency
4.3 nM [Ki]
4.4 nM [Ki]
1.7 nM [Ki]
4.8 nM [Ki]
3.8 nM [Ki]
101.0 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TOVLON
Palliative
Unknown
Palliative
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
14.6 ng/mL
30 mg single, rectal
MIANSERIN plasma
Homo sapiens
40.7 ng/mL
30 mg single, oral
MIANSERIN plasma
Homo sapiens
102 μg/L
60 mg single, oral
MIANSERIN plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
157.6 ng × h/mL
0.15 mg/kg single, intravenous
MIANSERIN plasma
Homo sapiens
275 ng × h/mL
30 mg single, oral
MIANSERIN plasma
Homo sapiens
541.8 ng × h/mL
30 mg single, rectal
MIANSERIN plasma
Homo sapiens
435.4 ng × h/mL
30 mg single, oral
MIANSERIN plasma
Homo sapiens
1356 μg × h/L
60 mg single, oral
MIANSERIN plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
9.6 h
0.15 mg/kg single, intravenous
MIANSERIN plasma
Homo sapiens
7.3 h
30 mg single, oral
MIANSERIN plasma
Homo sapiens
27 h
single, oral
MIANSERIN plasma
Homo sapiens
18.3 h
30 mg single, oral
MIANSERIN plasma
Homo sapiens
21 h
60 mg single, oral
MIANSERIN plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
10%
MIANSERIN plasma
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
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
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.
Substance Class Chemical
Record UNII
2X03TN217S
Record Status Validated (UNII)
Record Version