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

Stem definitionDrug idCAS RN
sulpiride derivatives and analogues 2365 80125-14-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • remoxipride
  • (S)-Remoxipride
  • remoxipride hydrochloride
  • remoxipride HCl
An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.
  • Molecular weight: 371.28
  • Formula: C16H23BrN2O3
  • CLOGP: 3.37
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 50.80
  • ALOGS: -3.47
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.30 g O
0.30 g P

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
ATC N05AL04 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Benzamides
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

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 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
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
117591-79-4 SECONDARY_CAS_RN
0223RD59PE UNII
235832 RXNORM
004031 NDDF
004032 NDDF
349884002 SNOMEDCT_US
419361008 SNOMEDCT_US
CHEMBL3989556 ChEMBL_ID
CHEMBL1899328 ChEMBL_ID

Pharmaceutical products:

None