Tegaserod

Serotonin-4 Receptor Agonist — ALIMENTARY TRACT AND METABOLISM

Key facts

Tegaserod is an ofm drug in the Serotonin-4 Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 2002. Its mechanism of action is classified as Serotonin 4 Receptor Agonists. DrugCentral lists 23 molecular targets, including HTR4, HTR2B and HTR4. Recorded indications include Chronic idiopathic constipation and Irritable bowel syndrome characterized by constipation.

• Approval status: ofm (first approved 2002 by the FDA).
• Drug class: Serotonin-4 Receptor Agonist.
• Mechanism of action: Serotonin 4 Receptor Agonists.
• Molecular targets: HTR4, HTR2B, HTR4 and HTR1D (23 listed in DrugCentral).
• Indications: Chronic idiopathic constipation and Irritable bowel syndrome characterized by constipation.
• ATC code: A06AX06 (Other drugs for constipation).
• Molecular formula: C16H23N5O; molecular weight 301.39 g/mol.

Indications & contraindications

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

Indications (2)

• Chronic idiopathic constipation
• Irritable bowel syndrome characterized by constipation

Contraindications (14)

• Acute nephropathy
• Adhesion of Gastrointestinal Tract
• Angina pectoris
• Breastfeeding (mother)
• Cerebrovascular accident
• Dehydration
• Diarrhea
• Disease of liver
• Disorder of biliary tract
• Disorder of gallbladder
• Hypovolemia
• Intestinal obstruction
• Ischemic colitis
• Myocardial infarction

Mechanism & targets

• Mechanism of action (MoA): Serotonin 4 Receptor Agonists
• Established pharmacologic class: Serotonin-4 Receptor Agonist

Molecular targets (23)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 4	HTR4	partial agonist	Ki 8.40
5-hydroxytryptamine receptor 2B	HTR2B	antagonist	Ki 8.40
5-hydroxytryptamine receptor 4	HTR4	unknown	EC50 7.90
5-hydroxytryptamine receptor 1D	HTR1D	unknown	Ki 7.30
Transmembrane protein 97	TMEM97	unknown	Ki 7.24
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 7.08
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.85
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 6.75
D(4) dopamine receptor	DRD4	unknown	Ki 6.72
5-hydroxytryptamine receptor 5A	HTR5A	unknown	Ki 6.70
D(2) dopamine receptor	DRD2	unknown	Ki 6.53
D(3) dopamine receptor	DRD3	unknown	Ki 6.37
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 6.37
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 6.25
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 5.79
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 5.79
5-hydroxytryptamine receptor 3A	HTR3A	unknown	Ki 5.60
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 5.58
Mu-type opioid receptor	OPRM1	unknown	Ki 5.55
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 5.55

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2002-07-24	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
A06AX06	ALIMENTARY TRACT AND METABOLISM › DRUGS FOR CONSTIPATION › DRUGS FOR CONSTIPATION › Other drugs for constipation

Chemical structure

• Molecular formula: C₁₆H₂₃N₅O
• Molecular weight: 301.39 g/mol
• CAS number: —
• InChIKey: IKBKZGMPCYNSLU-UHFFFAOYSA-N
• PubChem CID: 135409453

CCCCCNC(=N)NN=CC1=CNC2=C1C=C(OC)C=C2

Frequently asked questions

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

What is Tegaserod used for?

DrugCentral lists the following indications for Tegaserod: Chronic idiopathic constipation and Irritable bowel syndrome characterized by constipation.

How does Tegaserod work?

Tegaserod is classified as Serotonin 4 Receptor Agonists; its molecular targets in DrugCentral include HTR4 (partial agonist), HTR2B (antagonist), HTR4 and HTR1D.

When was Tegaserod first approved?

Tegaserod was first approved by the FDA in 2002.

What drug class does Tegaserod belong to?

Tegaserod is in the Serotonin-4 Receptor Agonist class.

What is the chemical formula of Tegaserod?

Tegaserod has the molecular formula C16H23N5O and a molecular weight of 301.39 g/mol.

Sources

• DrugCentral drug card 2579 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1516474 — compound record and bioactivity
• PubChem CID 135409453 — chemical identifiers
• DrugBank DB01079 — drug record
• FDA UNII 458VC51857 — substance identity
• DailyMed: FDA labels for Tegaserod — current prescribing information (label search)
• UniProt Q13639 (HTR4) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P28221 (HTR1D) — target protein
• UniProt Q5BJF2 (TMEM97) — target protein
• UniProt P08908 (HTR1A) — target protein
• UniProt P28335 (HTR2C) — target protein

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