mosapride ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
sulpiride derivatives and analogues 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 ยตM/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 78.98 23.75 42 4253 37100 63447627
Platelet count decreased 64.10 23.75 57 4238 116065 63368662
Interstitial lung disease 47.93 23.75 37 4258 61871 63422856
Anaemia 44.90 23.75 75 4220 293355 63191372
Altered state of consciousness 43.88 23.75 25 4270 25205 63459522
Upper respiratory tract inflammation 43.52 23.75 13 4282 2510 63482217
Ileus 38.05 23.75 19 4276 14706 63470021
Cerebral infarction 37.10 23.75 22 4273 23871 63460856
Renal impairment 36.54 23.75 37 4258 88318 63396409
Cardiac failure 32.68 23.75 35 4260 89107 63395620
Fatigue 32.44 23.75 10 4285 888018 62596709
Neutrophil count decreased 31.69 23.75 28 4267 56378 63428349
Decreased appetite 31.66 23.75 59 4236 250993 63233734
Hypokalaemia 31.62 23.75 37 4258 103767 63380960
Drug ineffective 31.26 23.75 16 4279 1044749 62439978
Pyrexia 30.66 23.75 85 4210 470393 63014334
Drug eruption 28.63 23.75 20 4275 28674 63456053
Alanine aminotransferase increased 28.34 23.75 35 4260 103735 63380992
Blood pressure decreased 28.29 23.75 28 4267 64994 63419733
Pneumonia aspiration 27.49 23.75 21 4274 34519 63450208
Aspartate aminotransferase increased 27.19 23.75 32 4263 90245 63394482
Pain 25.85 23.75 9 4286 740619 62744108
Drug-induced liver injury 24.67 23.75 21 4274 40201 63444526
White blood cell count decreased 24.55 23.75 38 4257 139066 63345661

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 83.89 20.25 53 3397 44310 34909171
Interstitial lung disease 71.89 20.25 56 3394 65226 34888255
Pneumonia aspiration 55.09 20.25 40 3410 41863 34911618
Cerebral infarction 42.55 20.25 29 3421 27426 34926055
Platelet count decreased 38.61 20.25 53 3397 119664 34833817
Pneumonia 38.11 20.25 99 3351 362528 34590953
Gastric cancer 29.89 20.25 14 3436 6455 34947026
Disseminated intravascular coagulation 24.57 20.25 19 3431 21797 34931684
Altered state of consciousness 23.76 20.25 19 3431 22874 34930607
Decreased appetite 23.39 20.25 51 3399 166341 34787140
Zinc deficiency 22.80 20.25 4 3446 46 34953435

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 150.45 18.29 93 7960 73014 79663321
Interstitial lung disease 105.87 18.29 89 7964 112511 79623824
Platelet count decreased 94.43 18.29 107 7946 194557 79541778
Cerebral infarction 73.90 18.29 50 8003 45626 79690709
Pneumonia aspiration 71.42 18.29 57 7996 66910 79669425
Altered state of consciousness 63.90 18.29 45 8008 43777 79692558
Ileus 52.97 18.29 33 8020 26178 79710157
Upper respiratory tract inflammation 50.61 18.29 18 8035 4017 79732318
Fatigue 44.88 18.29 19 8034 929708 78806627
Cardiac failure 44.84 18.29 66 7987 154776 79581559
Decreased appetite 44.29 18.29 103 7950 342315 79394020
Renal impairment 42.47 18.29 65 7988 157718 79578617
Pneumonia 41.23 18.29 153 7900 660093 79076242
Blood pressure decreased 40.39 18.29 50 8003 99416 79636919
Aspartate aminotransferase increased 38.56 18.29 58 7995 138583 79597752
Drug ineffective 35.85 18.29 34 8019 1080879 78655456
Pyrexia 33.32 18.29 146 7907 678563 79057772
Disseminated intravascular coagulation 32.94 18.29 28 8025 35814 79700521
Gastric cancer 31.74 18.29 17 8036 10162 79726173
Neutrophil count decreased 31.54 18.29 43 8010 93916 79642419
Drug-induced liver injury 31.39 18.29 36 8017 66081 79670254
Alanine aminotransferase increased 30.47 18.29 57 7996 162513 79573822
Drug eruption 29.92 18.29 29 8024 43906 79692429
White blood cell count decreased 28.07 18.29 60 7993 188228 79548107
Toxicity to various agents 26.95 18.29 5 8048 421535 79314800
Anaemia 25.93 18.29 101 7952 444914 79291421
Adrenocorticotropic hormone deficiency 24.52 18.29 8 8045 1377 79734958
Enterocolitis viral 24.15 18.29 6 8047 387 79735948
Liver disorder 24.08 18.29 33 8020 72384 79663951
Salivary hypersecretion 24.02 18.29 16 8037 14208 79722127
Malignant neoplasm progression 23.41 18.29 46 8007 135944 79600391
Mechanical ileus 23.36 18.29 7 8046 912 79735423
Zinc deficiency 23.22 18.29 5 8048 171 79736164
Blood urea increased 22.20 18.29 26 8027 48764 79687571
Pneumonia bacterial 21.76 18.29 17 8036 19314 79717021
Hypokalaemia 21.57 18.29 46 8007 143994 79592341
Pain 20.09 18.29 25 8028 703777 79032558
Pulmonary hypertension 19.23 18.29 24 8029 48056 79688279
Chronic gastritis 19.20 18.29 9 8044 4059 79732276
Colon cancer 19.06 18.29 14 8039 14509 79721826
White blood cell count increased 19.01 18.29 30 8023 74603 79661732
Idiopathic pulmonary fibrosis 18.87 18.29 9 8044 4219 79732116

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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