mianserin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1796 24219-97-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • mianserin hydrochloride
  • mianserin
  • mianserine
  • (+/-)-Mianserin
  • mianserine hydrochloride
  • mianserin HCl
  • mianserine HCl
A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.
  • Molecular weight: 264.37
  • Formula: C18H20N2
  • CLOGP: 3.76
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 6.48
  • ALOGS: -3.06
  • ROTB: 0

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 3.40 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 5 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 6.48 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 22 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 13.75 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 21.90 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 9.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1976 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Toxicity to various agents 258.03 59.97 74 403 32680 2324928
Fall 190.35 59.97 64 413 47035 2310573
Somnolence 114.34 59.97 37 440 23448 2334160
Hepatocellular injury 110.73 59.97 25 452 4030 2353578
Agranulocytosis 103.40 59.97 23 454 3459 2354149
Brain death 101.89 59.97 17 460 553 2357055
Cholestasis 101.88 59.97 23 454 3698 2353910
Hyponatraemia 98.61 59.97 29 448 13296 2344312
Hypotension 87.70 59.97 33 444 32403 2325205
Confusional state 81.42 59.97 29 448 24315 2333293
Overdose 67.54 59.97 24 453 19883 2337725

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Toxicity to various agents 69.02 58.02 26 232 29115 1717408
Confusional state 61.39 58.02 22 236 21256 1725267

Pharmacologic Action:

SourceCodeDescription
ATC N06AX03 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTIDEPRESSANTS
Other antidepressants
MeSH PA D018663 Adrenergic Agents
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35717 sedative
CHEBI has role CHEBI:37890 alpha-adrenergic antagonist
CHEBI has role CHEBI:35640 adrenergic uptake inhibitor
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:35678 histamine agonist
CHEBI has role CHEBI:37955 H1-receptor antagonist
MeSH PA D000928 Antidepressive Agents
MeSH PA D018687 Antidepressive Agents, Second-Generation
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Major depressive disorder indication 370143000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.2 Basic
pKa2 1.03 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 8.12 WOMBAT-PK IUPHAR
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 8.17 WOMBAT-PK IUPHAR
5-hydroxytryptamine receptor 2C GPCR ANTAGONIST Ki 8.52 WOMBAT-PK IUPHAR
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 7.50 IUPHAR
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 7.40 IUPHAR
Histamine H2 receptor GPCR Ki 6.00 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 6.46 DRUG MATRIX
Muscarinic acetylcholine receptor M2 GPCR Ki 6.42 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 6.53 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 6.54 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 6.64 DRUG MATRIX
5-hydroxytryptamine receptor 3A Ion channel Ki 6.21 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 5.55 CHEMBL
D(2) dopamine receptor GPCR Ki 5.66 CHEMBL
D(4) dopamine receptor GPCR IC50 5.48 CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 5.26 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 6.39 CHEMBL
5-hydroxytryptamine receptor 1F GPCR Ki 8.06 WOMBAT-PK
Alpha-2C adrenergic receptor GPCR Ki 8.42 WOMBAT-PK
5-hydroxytryptamine receptor 1D GPCR Ki 6.99 WOMBAT-PK
5-hydroxytryptamine receptor 1B GPCR Ki 7.53 WOMBAT-PK
Histamine H4 receptor GPCR EC50 6.12 WOMBAT-PK
Histamine H1 receptor GPCR Ki 9.25 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 7.57 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 7.06 WOMBAT-PK
5-hydroxytryptamine receptor 6 GPCR Ki 7.17 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 6.13 WOMBAT-PK
Sodium-dependent noradrenaline transporter Transporter Kd 7.15 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 8.32 WOMBAT-PK
D(1A) dopamine receptor GPCR Ki 6 WOMBAT-PK
Sodium-dependent dopamine transporter Transporter Ki 5.03 PDSP
Sodium-dependent serotonin transporter Transporter Ki 5.40 PDSP
Alpha-1B adrenergic receptor GPCR Ki 7.18 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter IC50 5.54 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR Ki 8.96 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR IC50 5.72 CHEMBL
Serotonin 3 receptor (5HT3) Ion channel Ki 6.60 CHEMBL
Alpha-1A adrenergic receptor GPCR IC50 10.15 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 7.21 CHEMBL
Serotonin 1 (5-HT1) receptor GPCR Ki 6.24 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.37 CHEMBL
Cerebral cortex alpha adrenergic receptor GPCR IC50 8.22 CHEMBL
5-hydroxytryptamine receptor 1B GPCR Ki 5.33 CHEMBL
D(1A) dopamine receptor GPCR Ki 5.85 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 7.77 CHEMBL
D(2) dopamine receptor GPCR Ki 6.08 CHEMBL
Serotonin 3 (5-HT3) receptor Ion channel Ki 7.15 CHEMBL
Transporter Transporter Ki 7.59 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 7.20 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 8.85 CHEMBL
G-protein coupled receptor Unclassified IC50 4.14 CHEMBL
D(3) dopamine receptor GPCR Ki 5.82 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 8.82 CHEMBL
Histamine H1 receptor GPCR Ki 9.07 CHEMBL
5-hydroxytryptamine receptor 1B Unclassified ANTAGONIST Ki 8.30 IUPHAR
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 7.40 IUPHAR
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 7 IUPHAR

External reference:

IDSource
C0700456 UMLSCUI
D01358 KEGG_DRUG
250PJI13LM UNII
2543 INN_ID
21535-47-7 SECONDARY_CAS_RN
18113 MMSL
96200003 SNOMEDCT_US
6929 RXNORM
387565003 SNOMEDCT_US
4027429 VANDF
004006 NDDF
CHEBI:51137 CHEBI
CHEMBL6437 ChEMBL_ID
CHEMBL544428 ChEMBL_ID
DB06148 DRUGBANK_ID
4184 PUBCHEM_CID
D008803 MESH_DESCRIPTOR_UI
135 IUPHAR_LIGAND_ID

Pharmaceutical products:

None