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dolasetron

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dolasetron Basic information

Product Name:
dolasetron
Synonyms:
  • (2alpha,6alpha,8alpha,9abeta)-Octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl-1H-indole-3-carboxylate
  • Dolasteron
  • Octahydro-3-oxo-2,6-Methano-2H-quinolizin-8-yl Ester
  • 1H-Indole-3-carboxylic acid, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, (2alpha,6alpha,8alpha,9abeta)-
  • Dolasetronum
  • Dolasetronum [inn-latin]
  • Hsdb 7565
  • Unii-82wi2L7Q6e
CAS:
115956-12-2
MF:
C19H20N2O3
MW:
324.37
Product Categories:
  • API
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
115956-12-2.mol
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dolasetron Chemical Properties

Melting point:
278 ºC
Boiling point:
535.1±50.0 °C(Predicted)
Density 
1.37±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,2-8°C
solubility 
Chloroform (Slightly), DMSO (Slightly), Methanol (Sparingly)
pka
15.36±0.30(Predicted)
form 
Solid
color 
White
Water Solubility 
Soluble
CAS DataBase Reference
115956-12-2
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Safety Information

Hazardous Substances Data
115956-12-2(Hazardous Substances Data)
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dolasetron Usage And Synthesis

Description

Dolasetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 20 nM). It is selective for 5-HT3 receptors over 5-HT1A, 5-HT1B, 5-HT2, dopamine D2, α1-, α2-, β-adrenergic, M1-5 muscarinic acetylcholine, and neurokinin-1 (NK1) receptors (IC50s = >10 μM for all). Dolasetron inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC50 = 3.8 nM). It increases the latency to emesis and reduces the number of vomiting and retching episodes induced by cisplatin in ferrets when administered at doses of 0.5 or 2 mg/kg. Formulations containing dolasetron have been used in the prevention of postoperative or chemotherapy-induced nausea.

Chemical Properties

White Solid

Uses

prevention and treatment of postoperative nausea and vomiting

Uses

Dolasetron is a bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist.It is used as antiemetic.

Uses

Bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist. Antiemetic.

Definition

ChEBI: LSM-5418 is an indolyl carboxylic acid.

brand name

Anzemet (Sanofi Aventis.

dolasetron Preparation Products And Raw materials

Preparation Products

dolasetronSupplier

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