molsidomine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
1831 25717-80-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • molsidomine
  • molsidolat
  • morsydomine
  • motazomin
  • molsidomin
A morpholinyl sydnone imine ethyl ester, having a nitrogen in place of the keto oxygen. It acts as NITRIC OXIDE DONORS and is a vasodilator that has been used in ANGINA PECTORIS.
  • Molecular weight: 242.24
  • Formula: C9H14N4O4
  • CLOGP: 0.56
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 0
  • TPSA: 72.60
  • ALOGS: -1.88
  • ROTB: 4

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 52 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 1 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.60 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAPK7,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PRKDC,SIK2,SIK3,STK33,TEK,TTK 33
kinase-selectivity-class AXL,BRAF,DDR1,EPHB4,GRK2,MAPK7,PRKDC,STK33,TEK,TTK 10
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

None

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
Toxic epidermal necrolysis 219.54 52.34 63 1971 32465 90593948
Mucosal erosion 109.96 52.34 21 2013 1824 90624589
Antinuclear antibody negative 109.21 52.34 16 2018 270 90626143
Coombs positive haemolytic anaemia 100.60 52.34 16 2018 474 90625939
Antiphospholipid syndrome 93.61 52.34 19 2015 2255 90624158
Dermatitis exfoliative 92.13 52.34 22 2012 5514 90620899
Herpes simplex reactivation 82.37 52.34 15 2019 1004 90625409
Gastritis haemorrhagic 79.81 52.34 16 2018 1784 90624629
Cholecystitis 75.86 52.34 24 2010 17016 90609397
Hyperthyroidism 74.17 52.34 24 2010 18286 90608127
Complex regional pain syndrome 73.59 52.34 16 2018 2643 90623770
Electrolyte imbalance 68.05 52.34 24 2010 23721 90602692
Conjunctivitis 65.29 52.34 24 2010 26682 90599731
Anxiety disorder 63.78 52.34 16 2018 4906 90621507
Respiratory disorder 59.43 52.34 29 2005 64787 90561626
Genital erosion 58.73 52.34 10 2024 453 90625960
Erysipelas 58.53 52.34 17 2017 9035 90617378
Multiple organ dysfunction syndrome 57.97 52.34 29 2005 68307 90558106
Fall 55.98 52.34 61 1973 481749 90144664
Product prescribing error 55.39 52.34 22 2012 30123 90596290
Erythema 53.80 52.34 43 1991 229203 90397210

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
General physical health deterioration 62.63 34.73 49 1560 151197 42468529
Oral mucosal eruption 54.83 34.73 10 1599 397 42619329
Pyelitis 42.50 34.73 7 1602 151 42619575
Syncope 36.33 34.73 30 1579 99376 42520350
Orthostatic intolerance 35.90 34.73 8 1601 875 42618851
Dizziness 35.23 34.73 45 1564 249209 42370517

FDA Adverse Event Reporting System (Geriatric)

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
Toxic epidermal necrolysis 164.05 33.68 62 3208 56665 110529364
Mucosal erosion 95.23 33.68 21 3249 2803 110583226
Product prescribing error 86.10 33.68 38 3232 51293 110534736
Electrolyte imbalance 70.54 33.68 30 3240 36998 110549031
Dermatitis exfoliative 70.44 33.68 22 3248 11325 110574704
Hyperthyroidism 56.70 33.68 24 3246 29237 110556792
Cholecystitis 56.11 33.68 23 3247 25859 110560170
Conjunctivitis 53.37 33.68 24 3246 33768 110552261
Genital erosion 50.37 33.68 10 3260 801 110585228
Respiratory disorder 49.21 33.68 29 3241 71353 110514676
Fall 46.74 33.68 72 3198 603410 109982619
Oral mucosal eruption 46.66 33.68 10 3260 1167 110584862
General physical health deterioration 45.11 33.68 59 3211 425236 110160793
Antinuclear antibody negative 44.42 33.68 7 3263 146 110585883
Blister 43.72 33.68 43 3227 227333 110358696
Stevens-Johnson syndrome 43.05 33.68 23 3247 46878 110539151
Antiphospholipid syndrome 39.07 33.68 10 3260 2513 110583516
Syncope 38.36 33.68 38 3232 202498 110383531
Erythema 38.20 33.68 45 3225 291402 110294627
Purpura 37.48 33.68 17 3253 24371 110561658
Pyelitis 37.23 33.68 7 3263 421 110585608
Cholelithiasis 36.60 33.68 23 3247 63399 110522630

FDA Adverse Event Reporting System (Pediatric)

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
Small for dates baby 16.84 16.83 7 4 3733 110209

Pharmacologic Action:

SourceCodeDescription
ATC C01DX12 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
VASODILATORS USED IN CARDIAC DISEASES
Other vasodilators used in cardiac diseases
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents
MeSH PA D020030 Nitric Oxide Donors
CHEBI has role CHEBI:22586 antioxidant
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:50566 nitric oxide donor
CHEBI has role CHEBI:68494 apoptosis inhibitor
CHEBI has role CHEBI:77307 cardioprotective agent

Related Drugs by ATC class:

C01DX Other vasodilators used in cardiac diseases 18 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Angina pectoris indication 194828000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.48 acidic
pKa2 6.72 Basic
pKa3 1.29 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
Estrogen receptor Nuclear hormone receptor IC50 4.61 CHEMBL

External reference:

IDSource
N0000167103 NUI
D01320 KEGG_DRUG
C0026400 UMLSCUI
CHEBI:31861 CHEBI
CHEMBL1329455 ChEMBL_ID
DB09282 DRUGBANK_ID
D008981 MESH_DESCRIPTOR_UI
5353788 PUBCHEM_CID
3125 INN_ID
D46583G77X UNII
7023 RXNORM
005842 NDDF
698196008 SNOMEDCT_US
D46583G77X INXIGHT DRUGS

Pharmaceutical products:

None