ALOSETRON

Alosetron is a selective 5‑HT3 receptor antagonist used for severe irritable bowel syndrome with diarrhea in women. Benefits include reduced urgency and abdominal discomfort. Risks include constipation, ischemic colitis, and serious gastrointestinal complications, requiring restricted use.

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Product Description


Mechanism of action

Alosetron is a highly selective antagonist of the serotonin 5-HT3 receptor, which is expressed on enteric neurons and visceral afferent fibres. By blocking these receptors in the gastrointestinal tract, alosetron reduces afferent signalling from the gut to the central nervous system, leading to decreased visceral pain perception, slower colonic transit and reduced intestinal secretion. This combination of effects helps normalise bowel frequency and stool consistency in patients with diarrhoea-predominant irritable bowel syndrome (IBS-D).

Benefits and advantages

The compound provides targeted symptom relief in carefully selected patients with severe, chronic IBS-D who have not responded adequately to conventional therapies. Clinical use has shown meaningful improvements in stool urgency, frequency, consistency and abdominal discomfort, which can significantly enhance quality of life. Because of its receptor selectivity, alosetron has minimal sedative or systemic neurological effects compared with less specific serotonergic agents.

Side effects and risks

The major safety concern with alosetron is the risk of serious gastrointestinal adverse events, including severe constipation, ischaemic colitis and, rarely, intestinal perforation. For this reason its therapeutic use is restricted to specific patient populations under strict prescribing programmes in clinical practice. Other adverse effects include abdominal pain, nausea and headache. As an active pharmaceutical ingredient, alosetron must be handled only by trained professionals under appropriate containment and safety procedures.

Datasheet


Molecular Formula

C17H18N4O

Molecular Weight

294.35 g/mol

CAS Number

122852-42-0

Storage Condition

Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light.

Solubility

4.38e-01 g/L

Purity

Purity information is available upon request (COA).

Synonym

alosetron; 122852-42-0; GR68755; alosetron monohydrochloride; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one

IUPAC/Chemical Name

5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one

InChl Key

JSWZEAMFRNKZNL-UHFFFAOYSA-N

InChl Code

InChI=1S/C17H18N4O/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2/h3-6,10H,7-9H2,1-2H3,(H,18,19)

References

https://pubchem.ncbi.nlm.nih.gov/compound/2099;

3D Conformer.

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