Scroll

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

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

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	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 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	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 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	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:

Source	Code	Description
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 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
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