General
Preferred name
TIAPRIDE
Synonyms
TIAPRIDE HYDROCHLORIDE ()
Tiapride (hydrochloride) ()
Luxoben ()
Tiapride hcl ()
Tiapridex ()
Italprid ()
Tiapridal ()
Gramalil ()
Sereprile ()
NSC-758225 ()
P&D ID
PD013238
CAS
51012-32-9
51012-33-0
Tags
drug candidate
natural product
drug
available
Drug indication
Alcohol dependence
Neuropathic pain
Drug Status
investigational
approved
Max Phase
Phase 3
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS
Tiapride has a high degree of regional selectivity for limbic areas. One study found that tiapride shows over three times as much affinity for limbic areas than striatal areas as opposed to the near equal selectivity for limbic and striatal regions shown by haloperidol.; Another study in rats found tiapride's affinity for the septum, a limbic region, to be over thirty times as high as for the striatum.; Efficacy at the D2 receptor is moderate, with 80 percent of receptors occupied even in the presence of excess tiapride concentrations.
MOA
Tiapride is a selective dopamine D2 and D3 receptor antagonist, offering an advantage over other neuroleptic drugs, such as haloperidol and risperidone, which bind a range of targets including four of the five known dopamine receptor subtypes (D1-4), serotonin (5-HT2A, 2C), α1- and α2-adrenergic, and histamine H1 receptors. Compared to these drugs, tiapride has a relatively moderate affinity for its target receptors, displacing 50 percent of 3H-raclopride binding at a concentration of 320 nM at D2 receptors and a concentration of 180 nM at D3 receptors.
ABSORPTION
The bioavailability of tiapride is approximately 75 percent. It has a Tmax is 0.4-1.5 hours and Tss is 24-48 hours with 3 time daily dosing. Benzamide and its derivatives are highly water-soluble but known to cross the blood-brain barrier, necessitating carrier-mediated transport.
DESCRIPTION
D2 and D3 dopamine receptor antagonist; antipsychotic
(LOPAC library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
19
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine BioReference Compounds
Ki Database
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
49
Molecular Weight
328.15
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
1
Aromatic Ring Count
1
cLogP
1.17
TPSA
75.71
Fraction CSP3
0.53
Chiral centers
0.0
Largest ring
6.0
QED
0.78
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
D2/D3
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Target
D2
D3
DRD2, DRD3
Dopamine Receptor
Indication
dyskinesia, abstinence from alcohol, psychosis
MOA
Dopamine Receptor antagonist
Source data
