Thiethylperazine

Summary

Thiethylperazine (CHEMBL1378) is an approved small-molecule phenothiazine antipsychotic drug (ATC R06AD03); indicated across 3 conditions including allergic disease and alzheimer disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AD03
• Indications: 3 conditions
• Clinical trials: 1
• Chemistry: 399.6 Da · C22H29N3S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1378
Name	Thiethylperazine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5440
ChEBI	CHEBI:9544
ATC	R06AD03
Molecular formula	C22H29N3S2
Molecular weight	399.6
InChIKey	XCTYLCDETUVOIP-UHFFFAOYSA-N

SMILES: CCSC1=CC2=C(C=C1)SC3=CC=CC=C3N2CCCN4CCN(CC4)C

IUPAC name: 2-ethylsulfanyl-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine

ChEBI definition: A member of the class of phenothiazines that is perazine substituted by a ethylsulfanyl group at position 2.

Pharmacological roles (ChEBI): phenothiazine antipsychotic drug, histamine antagonist, muscarinic antagonist, serotonergic antagonist, dopaminergic antagonist, antiemetic.

Also known as: Thiethylperazine, Tietilperazina, THIETHYLPERAZINE, thiethylperazine

Parent form; salt/anhydrous children: CHEMBL1200856, CHEMBL1201074, CHEMBL1326247, CHEMBL2359670, CHEMBL3989478

Patent coverage: 1,535 distinct patent families (6,185 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 6,091 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 25 (assay-derived). Sample: Pleiotropic ABC efflux transporter of multiple drugs, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, D(1A) dopamine receptor, Thromboxane A2 receptor, Progesterone receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 29 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD3	8.51	AC50	3.1	nM	CHEMBL_ACT_25195094
DRD1	8.1	AC50	7.9	nM	CHEMBL_ACT_25115799
DRD2	7	AC50	100	nM	CHEMBL_ACT_25140998
HRH1	6.77	AC50	170	nM	CHEMBL_ACT_25213184
ADRA2A	6.68	AC50	210.7	nM	CHEMBL_ACT_25157018
HTR1A	6.35	AC50	449.3	nM	CHEMBL_ACT_25165613
KCNH2	5.92	AC50	1200	nM	CHEMBL_ACT_25118816
ADRA1A	5.8	AC50	1600	nM	CHEMBL_ACT_25218554
HTR2A	5.8	AC50	1600	nM	CHEMBL_ACT_25225784
SLC6A2	5.78	AC50	1654	nM	CHEMBL_ACT_25146589
ADRA2C	5.66	AC50	2200	nM	CHEMBL_ACT_25148550
CHRM2	5.65	AC50	2239	nM	CHEMBL_ACT_25196325
P33302	5.64	IC50	2300	nM	CHEMBL_ACT_5306643
OPRM1	5.57	AC50	2688	nM	CHEMBL_ACT_25158764
SLC6A3	5.41	AC50	3869	nM	CHEMBL_ACT_25125548
TBXA2R	5.4	AC50	3976	nM	CHEMBL_ACT_25198432
SLC6A4	5.31	AC50	4875	nM	CHEMBL_ACT_25151916
ADORA3	5.18	AC50	6617	nM	CHEMBL_ACT_25199192
SLC6A2	5.02	AC50	9600	nM	CHEMBL_ACT_25145651

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
allergic disease	4	MONDO:0005271	MONDO:0005271
Alzheimer disease	2	MONDO:0004975	MONDO:0004975

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07084753	Not specified	NOT_YET_RECRUITING	Non-opioid Anesthesia Based on Thoracic Paravertebral Block During Laparoscopic Sleeve Gastrectomy

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).