Tiapride

N05L - N05L ATC N05AL03 Small molecule Natural product

JFDA label: TIAPRIDAL TAB

Mechanism of Action

Antagonist of D(3) dopamine receptor — Dopamine D3 receptor antagonist; Antagonist of D(2) dopamine receptor — Dopamine D2 receptor antagonist

Target	Action	Gene / class
D(2) dopamine receptor efficacy	ANTAGONIST	DRD2
D(3) dopamine receptor efficacy	ANTAGONIST	DRD3

Indications

Off-label

Anxiety
Dementia
Depressive Disorder
Psychotic Disorders
Schizophrenia
Tic Disorders
Tourette Syndrome

Chemistry & Properties

Formula	C15H24N2O4S
Molecular weight	328.43 g/mol
IUPAC name	N-[2-(diethylamino)ethyl]-2-methoxy-5-methylsulfonylbenzamide
CAS	51012-32-9
PubChem CID	5467
InChIKey	`JTVPZMFULRWINT-UHFFFAOYSA-N`
logP	1.17 (XLogP 0.9)
Polar surface area	75.71 Å²
H-bond acceptors / donors	5 / 1
Drug-likeness (QED)	0.78
Lipinski violations	0

SMILES

CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes

Enzyme interactions

Enzyme	Role	Detail
CYP2C19	Substrate	—

Receptor binding (top 3)

Target	Action	Affinity
DOPAMINE D4 (DRD4)	Binding	pKi 7.9
DOPAMINE D2 (DRD2)	Binding	pKi 7.1
DOPAMINE D3 (DRD3)	Binding	pKi 6.8

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (2)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
TIAPRIDAL TAB	Tablet 100 mg	20 tab	Ulfa Pharma Co.	2.020
TIAPRIDAL AMP	Ampoule 100 mg	12 amp	Ulfa Pharma Co.	2.830