Sertindole

NERVOUS SYSTEM

Key facts

Sertindole is a drug catalogued in DrugCentral. It was first approved by the UK Medicines and Healthcare Products Regulatory Agency (MHRA) in 1996. DrugCentral lists 33 molecular targets, including HTR2C, Htr2a and ADRA1B. Recorded indications include Schizophrenia.

• Molecular targets: HTR2C, Htr2a, ADRA1B and ADRA1A (33 listed in DrugCentral).
• Indications: Schizophrenia.
• ATC code: N05AE03 (Indole derivatives).
• Molecular formula: C24H26ClFN4O; molecular weight 440.95 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Schizophrenia

Mechanism & targets

Molecular targets (33)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 2C	HTR2C	inverse agonist	Ki 9.70
5-hydroxytryptamine receptor 2A	Htr2a	unknown	Ki 9.70
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 9.48
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 9.43
Serotonin 2 (5-HT2) receptor	Htr2c|Htr2a|Htr2b	unknown	IC50 9.41
D(2) dopamine receptor	DRD2	antagonist	Ki 9.35
D(2) dopamine receptor	Drd2	unknown	Ki 9.35
5-hydroxytryptamine receptor 2C	Htr2c	unknown	Ki 9.29
Histamine H1 receptor	HRH1	unknown	Ki 9.29
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 9.22
Alpha-1D adrenergic receptor	Adra1d	unknown	Ki 9.18
Adrenergic receptor alpha-1	Adra1b|Adra1d|Adra1a	unknown	Ki 8.85
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 8.74
D(3) dopamine receptor	DRD3	unknown	Ki 8.59
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 8.57
Alpha-1A adrenergic receptor	Adra1a	unknown	IC50 8.47
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 8.30
D(4) dopamine receptor	DRD4	unknown	Ki 7.96
D(1A) dopamine receptor	Drd1	unknown	Ki 7.92
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 7.55

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1996-05-23	UK Medicines and Healthcare Products Regulatory Agency (MHRA)	—	H. Lundbeck A/S

ATC classification

ATC code	Therapeutic hierarchy
N05AE03	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Indole derivatives

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• Swissmedic label: CYP2D6 · Actionable PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Drug interaction	71.8

Chemical structure

• Molecular formula: C₂₄H₂₆ClFN₄O
• Molecular weight: 440.95 g/mol
• CAS number: —
• InChIKey: GZKLJWGUPQBVJQ-UHFFFAOYSA-N
• PubChem CID: 60149

FC1=CC=C(C=C1)N1C=C(C2CCN(CCN3CCNC3=O)CC2)C2=C1C=CC(Cl)=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Sertindole used for?

DrugCentral lists the following indications for Sertindole: Schizophrenia.

How does Sertindole work?

Its molecular targets in DrugCentral include HTR2C (inverse agonist), Htr2a, ADRA1B and ADRA1A.

When was Sertindole first approved?

Sertindole was first approved by the UK Medicines and Healthcare Products Regulatory Agency (MHRA) in 1996.

What is the chemical formula of Sertindole?

Sertindole has the molecular formula C24H26ClFN4O and a molecular weight of 440.95 g/mol.

Sources

• DrugCentral drug card 2435 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL12713 — compound record and bioactivity
• PubChem CID 60149 — chemical identifiers
• DrugBank DB06144 — drug record
• FDA UNII GVV4Z879SP — substance identity
• UniProt P28335 (HTR2C) — target protein
• UniProt P14416 (DRD2) — target protein
• UniProt P35367 (HRH1) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P35348 (ADRA1A) — target protein
• UniProt P35462 (DRD3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.