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Stem definition	Drug id	CAS RN
sulpiride derivatives and analogues	1848	112885-41-3

Description:

Molecule	Description
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

Molecule

Description

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:

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC	20
kinase-selectivity-class	AXL,BRAF,CDK9,GRK2,SIK2,SIK3,TEK	7
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1998	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hepatic function abnormal	103.19	21.36	52	5403	46236	90576756
Platelet count decreased	77.76	21.36	65	5390	136904	90486088
Anaemia	57.33	21.36	87	5368	352715	90270277
Hypokalaemia	56.02	21.36	53	5402	131063	90491929
Interstitial lung disease	53.42	21.36	41	5414	76364	90546628
Upper respiratory tract inflammation	53.21	21.36	15	5440	2657	90620335
Renal impairment	51.61	21.36	46	5409	105375	90517617
Decreased appetite	49.05	21.36	84	5371	376456	90246536
Altered state of consciousness	46.64	21.36	27	5428	31505	90591487
Cerebral infarction	45.36	21.36	25	5430	26571	90596421
Neutrophil count decreased	42.73	21.36	35	5420	71497	90551495
Pyrexia	42.16	21.36	110	5345	660375	89962617
Drug eruption	41.22	21.36	26	5429	35381	90587611
Ileus	41.03	21.36	20	5435	16526	90606466
Cardiac failure	40.64	21.36	41	5414	109455	90513537
Pneumonia aspiration	40.16	21.36	27	5428	40913	90582079
Blood pressure decreased	39.29	21.36	34	5421	74861	90548131
Aspartate aminotransferase increased	37.21	21.36	38	5417	102899	90520093
Fatigue	36.70	21.36	12	5443	1154011	89468981
Alanine aminotransferase increased	36.25	21.36	40	5415	118298	90504694
White blood cell count decreased	34.11	21.36	46	5409	167063	90455929
Drug ineffective	33.74	21.36	21	5434	1384277	89238715
Pain	28.88	21.36	12	5443	996329	89626663
Gamma-glutamyltransferase increased	25.71	21.36	20	5435	37932	90585060
Ascites	25.69	21.36	22	5433	47718	90575274
Blood bilirubin increased	23.32	21.36	20	5435	43450	90579542
Concomitant disease aggravated	22.92	21.36	12	5443	11506	90611486
Enterocolitis viral	22.27	21.36	5	5450	352	90622640
Diarrhoea	21.39	21.36	112	5343	939078	89683914

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hepatic function abnormal	82.61	20.89	56	4241	51511	42565527
Interstitial lung disease	78.08	20.89	64	4233	78398	42538640
Pneumonia aspiration	69.93	20.89	50	4247	50028	42567010
Pneumonia	48.72	20.89	121	4176	422028	42195010
Cerebral infarction	43.19	20.89	31	4266	31138	42585900
Platelet count decreased	40.20	20.89	59	4238	138522	42478516
Delirium	38.41	20.89	36	4261	52483	42564555
Decreased appetite	35.53	20.89	67	4230	193070	42423968
Gastric cancer	28.74	20.89	14	4283	6889	42610149
Ileus	26.42	20.89	19	4278	19120	42597918
Disseminated intravascular coagulation	26.24	20.89	21	4276	24773	42592265
Aspartate aminotransferase increased	24.01	20.89	34	4263	77129	42539909
Altered state of consciousness	23.21	20.89	21	4276	29238	42587800
Neutrophil count decreased	21.30	20.89	29	4268	63386	42553652
Renal impairment	21.17	20.89	39	4258	110189	42506849

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hepatic function abnormal	174.79	18.42	106	9964	89189	110490040
Interstitial lung disease	121.60	18.42	101	9969	139233	110439996
Platelet count decreased	110.72	18.42	120	9950	230323	110348906
Pneumonia aspiration	106.36	18.42	75	9995	81158	110498071
Cerebral infarction	84.90	18.42	55	10015	51783	110527446
Decreased appetite	69.18	18.42	141	9929	475705	110103524
Renal impairment	66.80	18.42	84	9986	188361	110390868
Ileus	66.61	18.42	39	10031	30690	110548539
Altered state of consciousness	65.81	18.42	49	10021	57577	110521652
Pneumonia	57.85	18.42	193	9877	876521	109702708
Aspartate aminotransferase increased	56.20	18.42	71	9999	159865	110419364
Upper respiratory tract inflammation	54.86	18.42	19	10051	4352	110574877
Cardiac failure	53.20	18.42	75	9995	187551	110391678
Neutrophil count decreased	52.85	18.42	60	10010	120881	110458348
Fatigue	48.89	18.42	25	10045	1215933	109363296
Blood pressure decreased	48.43	18.42	56	10014	115035	110464194
Alanine aminotransferase increased	45.62	18.42	69	10001	183704	110395525
Hypokalaemia	44.58	18.42	68	10002	182380	110396849
White blood cell count decreased	44.50	18.42	77	9993	229313	110349916
Drug ineffective	43.32	18.42	45	10025	1520495	109058734
Drug eruption	42.85	18.42	37	10033	53622	110525607
Pyrexia	39.57	18.42	174	9896	898091	109681138
Anaemia	37.35	18.42	122	9948	546964	110032265
Disseminated intravascular coagulation	36.10	18.42	30	10040	41256	110537973
Gastric cancer	35.00	18.42	18	10052	10990	110568239
Drug-induced liver injury	28.25	18.42	44	10026	120023	110459206
Pain	27.40	18.42	28	10042	954927	109624302
Ascites	26.13	18.42	37	10033	92771	110486458
Mechanical ileus	25.97	18.42	8	10062	1269	110577960
Blood urea increased	25.24	18.42	28	10042	54929	110524300
Hyperuricaemia	25.22	18.42	16	10054	14515	110564714
Delirium	24.45	18.42	44	10026	134981	110444248
Malignant neoplasm progression	24.41	18.42	51	10019	174516	110404713
Enterocolitis viral	24.37	18.42	7	10063	874	110578355
Drug hypersensitivity	23.83	18.42	6	10064	454084	110125145
Constipation	23.66	18.42	79	9991	357707	110221522
Enterocolitis	23.63	18.42	17	10053	18932	110560297
Pulmonary hypertension	23.43	18.42	27	10043	55193	110524036
Cholecystitis	23.03	18.42	19	10051	25863	110553366
Pneumonia bacterial	22.79	18.42	19	10051	26242	110552987
Gamma-glutamyltransferase increased	22.76	18.42	28	10042	61281	110517948
Salivary hypersecretion	22.58	18.42	16	10054	17405	110561824
Infusion related reaction	22.11	18.42	4	10066	381158	110198071
Peripheral swelling	21.86	18.42	5	10065	404029	110175200
Adrenocorticotropic hormone deficiency	21.77	18.42	8	10062	2174	110577055
Diarrhoea	21.56	18.42	177	9893	1139328	109439901
Confusional state	21.34	18.42	8	10062	468672	110110557
Hypoalbuminaemia	21.16	18.42	19	10051	28955	110550274
Colon cancer	21.07	18.42	15	10055	16428	110562801
Lymphocyte count decreased	21.02	18.42	26	10044	57217	110522012
Urinary tract infection	20.65	18.42	71	9999	326211	110253018
Zinc deficiency	20.19	18.42	5	10065	354	110578875
Swelling	19.69	18.42	4	10066	351037	110228192
Blood bilirubin increased	19.51	18.42	29	10041	75943	110503286
Cholangitis acute	19.03	18.42	7	10063	1906	110577323
Cholangitis	18.88	18.42	14	10056	16321	110562908
Concomitant disease aggravated	18.86	18.42	14	10056	16350	110562879

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A03FA09	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS PROPULSIVES Propulsives
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D017366	Serotonin Receptor Agonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
CHEBI has role	CHEBI:35941	serotonergic agonist
CHEBI has role	CHEBI:50503	laxative
CHEBI has role	CHEBI:53784	antispasmodic drug
CHEBI has role	CHEBI:55324	gastrointestinal drug

Related Drugs by ATC class:

A03FA Propulsives 9 drugs

acotiamide alizapride bromopride cinitapride cisapride clebopride domperidone itopride metoclopramide

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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 4	GPCR	Q13639	5HT4R_HUMAN	AGONIST	Ki	6.90	IUPHAR	SCIENTIFIC LITERATURE
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.86	DRUG MATRIX
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.89	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.32	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6.16	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.69	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.73	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.06	DRUG MATRIX
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN		Ki	5.70	WOMBAT-PK
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	6	DRUG MATRIX
Cytochrome P450 1A2	Enzyme	P05177	CP1A2_HUMAN		IC50	6.40	DRUG MATRIX
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	6	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.68	DRUG MATRIX
5-hydroxytryptamine receptor 4	GPCR		5HT4R_CAVPO		Ki	7.16	CHEMBL
Serotonin 3 (5-HT3) receptor	Ion channel		5HT3A_RAT 5HT3B_RAT		Ki	5.92	CHEMBL

External reference:

ID	Source
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
I8MFJ1C0BY	UNII
135091	RXNORM
008862	NDDF
017672	NDDF
1163443001	SNOMEDCT_US
1172819001	SNOMEDCT_US
1172822004	SNOMEDCT_US
636582-62-2	SECONDARY_CAS_RN
I8MFJ1C0BY	INXIGHT DRUGS

Pharmaceutical products:

None

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

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: