Alosetron (hydro<wbr/>chloride)

Alosetron (hydrochloride)

CAT N°: 22434
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Alosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Kis = 0.3 and 0.4 nM for the rat cortical and human recombinant receptors, respectively).{39117} It is selective for 5-HT3 over 5-HT2 and 5-HT1A receptors (Kis = 6.3 and >100 µM, respectively), as well as ?1-, ?1-, and ?2- adrenergic, M1, M2, and M3 muscarinic, GABAA, dopamine D2, and nicotinic receptors at 10 ?M.{39120} Alosetron (0.3-10 nM) inhibits 5-HT-induced depolarization of isolated rat vagus nerve.{39117} It reduces wrap restraint stress-induced defecation and the number of abdominal muscle contractions in a rat model of irritable bowel syndrome with diarrhea (IBS-D) when administered at a dose of 0.1 mg/kg.{39118} Formulations containing alosetron have been used in the treatment of diarrhea-predominant irritable bowel syndrome in women.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-1H-pyrido[4,3-b]indol-1-one, monohydrochloride
  • Correlated keywords
    • 122852-42-0 5HT GR68755 IBSD
  • Product Overview:
    Alosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Kis = 0.3 and 0.4 nM for the rat cortical and human recombinant receptors, respectively).{39117} It is selective for 5-HT3 over 5-HT2 and 5-HT1A receptors (Kis = 6.3 and >100 µM, respectively), as well as ?1-, ?1-, and ?2- adrenergic, M1, M2, and M3 muscarinic, GABAA, dopamine D2, and nicotinic receptors at 10 ?M.{39120} Alosetron (0.3-10 nM) inhibits 5-HT-induced depolarization of isolated rat vagus nerve.{39117} It reduces wrap restraint stress-induced defecation and the number of abdominal muscle contractions in a rat model of irritable bowel syndrome with diarrhea (IBS-D) when administered at a dose of 0.1 mg/kg.{39118} Formulations containing alosetron have been used in the treatment of diarrhea-predominant irritable bowel syndrome in women.

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