mosapride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
sulpiride derivatives 1848 112885-41-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gasmotin
  • AS 4370
  • mosapride citrate hydrate
  • mosapride
  • mosapride citrate
  • mosapride citrate dihydrate
  • AS-4370
Mosapride is a 5-HT4 receptor agonist which increases the release of acetylcholine and stimulates GI motility.
  • Molecular weight: 421.90
  • Formula: C21H25ClFN3O3
  • CLOGP: 3.35
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 76.82
  • ALOGS: -4.29
  • ROTB: 7

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.35 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1998 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
Hepatic function abnormal 63.23 22.30 36 3771 32645 50568672
Platelet count decreased 50.27 22.30 49 3758 100677 50500640
Altered state of consciousness 44.70 22.30 25 3782 21885 50579432
Interstitial lung disease 40.75 22.30 33 3774 53143 50548174
Anaemia 40.65 22.30 70 3737 252386 50348931
Upper respiratory tract inflammation 38.61 22.30 12 3795 2377 50598940
Ileus 35.15 22.30 18 3789 13211 50588106
Cerebral infarction 34.41 22.30 21 3786 21583 50579734
Cardiac failure 30.65 22.30 33 3774 76007 50525310
Fatigue 30.34 22.30 8 3799 707593 49893724
Drug ineffective 30.33 22.30 12 3795 819321 49781996
Neutrophil count decreased 29.95 22.30 26 3781 46000 50555317
Renal impairment 29.04 22.30 32 3775 75629 50525688
Pyrexia 28.17 22.30 77 3730 380126 50221191
Blood pressure decreased 27.48 22.30 27 3780 55882 50545435
Decreased appetite 26.31 22.30 51 3756 200872 50400445
Pneumonia aspiration 25.35 22.30 20 3787 30984 50570333
White blood cell count decreased 25.10 22.30 37 3770 116685 50484632
Alanine aminotransferase increased 25.02 22.30 32 3775 88327 50512990
Aspartate aminotransferase increased 24.90 22.30 30 3777 77968 50523349
Hypokalaemia 23.56 22.30 31 3776 87961 50513356

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
Hepatic function abnormal 76.72 21.32 48 2890 39211 29532378
Interstitial lung disease 62.18 21.32 49 2889 57669 29513920
Pneumonia aspiration 52.54 21.32 37 2901 36700 29534889
Cerebral infarction 40.33 21.32 27 2911 24648 29546941
Platelet count decreased 33.02 21.32 46 2892 104626 29466963
Pneumonia 31.86 21.32 86 2852 320086 29251503
Gastric cancer 30.49 21.32 13 2925 4781 29566808
Disseminated intravascular coagulation 23.72 21.32 18 2920 19962 29551627

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
Hepatic function abnormal 126.89 18.51 82 6966 64231 64427453
Interstitial lung disease 88.10 18.51 78 6970 97654 64394030
Platelet count decreased 75.15 18.51 92 6956 167619 64324065
Pneumonia aspiration 67.16 18.51 54 6994 59217 64432467
Cerebral infarction 65.69 18.51 46 7002 40998 64450686
Altered state of consciousness 59.54 18.51 42 7006 37860 64453824
Ileus 49.50 18.51 31 7017 22935 64468749
Upper respiratory tract inflammation 46.62 18.51 17 7031 3765 64487919
Fatigue 43.43 18.51 14 7034 748716 63742968
Blood pressure decreased 38.07 18.51 47 7001 86152 64405532
Cardiac failure 37.15 18.51 58 6990 132315 64359369
Drug ineffective 35.94 18.51 24 7024 840223 63651461
Decreased appetite 35.54 18.51 88 6960 281201 64210483
Pneumonia 35.08 18.51 137 6911 559439 63932245
Gastric cancer 34.58 18.51 16 7032 6477 64485207
Pyrexia 34.39 18.51 136 6912 558508 63933176
Disseminated intravascular coagulation 31.47 18.51 27 7021 32321 64459363
Renal impairment 30.93 18.51 54 6994 134963 64356721
Neutrophil count decreased 30.76 18.51 40 7008 77156 64414528
Aspartate aminotransferase increased 30.20 18.51 50 6998 119738 64371946
White blood cell count decreased 28.50 18.51 57 6991 157780 64333904
Drug-induced liver injury 27.79 18.51 30 7018 47613 64444071
Anaemia 26.38 18.51 96 6952 378584 64113100
Enterocolitis viral 25.00 18.51 6 7042 309 64491375
Alanine aminotransferase increased 24.84 18.51 50 6998 138981 64352703
Toxicity to various agents 24.45 18.51 5 7043 363508 64128176
Drug eruption 23.29 18.51 24 7024 36112 64455572
Pneumonia bacterial 22.08 18.51 16 7032 15019 64476665
Mechanical ileus 21.01 18.51 6 7042 610 64491074
Malignant neoplasm progression 20.64 18.51 41 7007 112830 64378854
Salivary hypersecretion 20.36 18.51 14 7034 12099 64479585
Liver disorder 20.25 18.51 27 7021 53324 64438360
Idiopathic pulmonary fibrosis 19.11 18.51 9 7039 3791 64487893
Adrenocorticotropic hormone deficiency 19.04 18.51 6 7042 854 64490830
White blood cell count increased 18.60 18.51 29 7019 65985 64425699

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A03FA09 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
PROPULSIVES
Propulsives
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D017366 Serotonin Receptor Agonists
CHEBI has role CHEBI:35941 serotonin agonists
CHEBI has role CHEBI:55324 gastrointestinal drugs

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.95 Basic
pKa2 1.11 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 4 GPCR AGONIST Ki 6.90 IUPHAR SCIENTIFIC LITERATURE
Alpha-2A adrenergic receptor GPCR Ki 5.86 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.89 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.32 CHEMBL
Cytochrome P450 3A4 Enzyme IC50 6.16 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 5.69 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 6.73 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.06 DRUG MATRIX
5-hydroxytryptamine receptor 3A Ion channel Ki 5.70 WOMBAT-PK
Cytochrome P450 2C9 Enzyme IC50 6 DRUG MATRIX
Cytochrome P450 1A2 Enzyme IC50 6.40 DRUG MATRIX
Cytochrome P450 2C19 Enzyme IC50 6 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.68 DRUG MATRIX
5-hydroxytryptamine receptor 4 GPCR Ki 7.16 CHEMBL
Serotonin 3 (5-HT3) receptor Ion channel Ki 5.92 CHEMBL

External reference:

IDSource
D01994 KEGG_DRUG
112885-42-4 SECONDARY_CAS_RN
C0526501 UMLSCUI
CHEBI:94373 CHEBI
CHEMBL60889 ChEMBL_ID
CHEMBL1733174 ChEMBL_ID
DB11675 DRUGBANK_ID
C062720 MESH_SUPPLEMENTAL_RECORD_UI
119584 PUBCHEM_CID
242 IUPHAR_LIGAND_ID
6855 INN_ID
636582-62-2 SECONDARY_CAS_RN
I8MFJ1C0BY UNII
135091 RXNORM
008862 NDDF
017672 NDDF
1163443001 SNOMEDCT_US
1172819001 SNOMEDCT_US
1172822004 SNOMEDCT_US

Pharmaceutical products:

None