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remoxipride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sulpiride derivatives and analogues | 2365 | 80125-14-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
| 0.30 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.65 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.16 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5.50 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 40.77 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.821 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.122 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 23.878 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 12.474 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 73.900 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 76.970 | % | High | 1 |
| herg | hERG pIC50 | 4.895 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.421 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 11.194 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 69.030 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ZAP70 | 51 | |||
| kinase-selectivity-class | AXL,EIF2AK3,EPHB4,GRK2,SIK2 | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.104 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 80.910 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 75.760 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.164 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 83.960 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 159.221 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 91.830 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 71.850 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 939.723 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1990 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AL04 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Benzamides |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014150 | Antipsychotic Agents |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018492 | Dopamine Antagonists |
Related Drugs by ATC class:
N05AL Benzamides 6 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 | 13.44 | acidic |
| pKa2 | 9.09 | 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]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | GPCR | ANTAGONIST | IC50 | 6.06 | CHEMBL | KEGG DRUG | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.26 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Kd | 5.40 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 5.51 | PDSP | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.16 | PDSP | |||||
| D(4) dopamine receptor | GPCR | Ki | 5.41 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | IC50 | 5.85 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Ki | 6.06 | CHEMBL | |||||
| D(3) dopamine receptor | GPCR | Ki | 5.34 | CHEMBL | |||||
| Dopamine receptor | GPCR | IC50 | 5.80 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166887 | NUI |
| D02682 | KEGG_DRUG |
| C0073047 | UMLSCUI |
| CHEBI:92948 | CHEBI |
| CHEMBL22242 | ChEMBL_ID |
| DB00409 | DRUGBANK_ID |
| D017330 | MESH_DESCRIPTOR_UI |
| 54477 | PUBCHEM_CID |
| 5197 | INN_ID |
| 0223RD59PE | UNII |
| 235832 | RXNORM |
| 004031 | NDDF |
| 004032 | NDDF |
| 349884002 | SNOMEDCT_US |
| 419361008 | SNOMEDCT_US |
| CHEMBL3989556 | ChEMBL_ID |
| 117591-79-4 | SECONDARY_CAS_RN |
| 0223RD59PE | INXIGHT DRUGS |
Pharmaceutical products:
None