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Dolasetron mesylate

pharmaceutical raw materials
Dolasetron mesylate structure

Dolasetron mesylate 

structure
  • CAS No:

    115956-13-3

  • Formula:

    C19H20N2O3.CH4O3S

  • Chemical Name:

    Dolasetron mesylate

  • Synonyms:

    1H-Indole-3-carboxylic acid,octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester,stereoisomer,methanesulfonate (1:1);1H-Indole-3-carboxylic acid,octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester,(2α,6α,8α,9aβ)-,monomethanesulfonate;1H-Indole-3-carboxylic acid,octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester,stereoisomer,monomethanesulfonate;2,6-Methano-2H-quinolizine,1H-indole-3-carboxylic acid deriv.;MDL 73147EF;Dolasetron mesylate;Anzemet;Anxemet;126126-99-6

  • Categories:

    Active Pharmaceutical Ingredients  >  Digestive System Drugs

Description

Dolasetron was launched as Anzemet in Australia and the US for the prevention of nausea and vomiting in chemotherapy patients. It is a highly potent and very selective antagonist of 5-HT3 receptors ; it is the sixth in this class of compounds to be marketed for the treatment of chemotherapy-induced emesis. The last two approved in this class were Nazasetron (1994) and Ramosetron (1996). Anzemet was prepared by a seven step sequence from a cyclopentenecarboxylic ester via a Robinson-Schopf

Dolasetron mesylate Basic Attributes

438.49

420.135508

214-599-3

DTXSID3046827

Characteristics

134.38000

2.97740

278 °C

535.1ºC at 760 mmHg

277.4ºC

H2O: >30mg/mL

2-8°C

Safety Information

3

R20/21/22

Drug Information

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS. (See all compounds classified as Serotonin Antagonists.)|Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)

1H-indole-3-carboxylic acid, (6R,9AS)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, rel-, methanesulfonate, hydrate (1:1:1)

Dolasetron mesylate Use and Manufacturing

Uses

Antidepressant

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:420.5
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:3
Exact Mass:420.13550766
Monoisotopic Mass:420.13550766
Topological Polar Surface Area:125
Heavy Atom Count:29
Complexity:627
Defined Atom Stereocenter Count:1
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Selective 5-HT3 receptor antagonists inhibit nausea and vomiting by antagonizing 5-HT3 receptors in peripheral vagal nerve endings and central emetic chemoreceptor areas. They can cause acute, usually reversible, electrocardiographic changes (PR and QTc prolongation; QRS widening).

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Registered Holders

  • EMCURE PHARMACEUTICALS LTD

    United States United States
    Active
  • USV PRIVATE LIMITED

    India India
    Active
  • Haisco Pharmaceutical(Meishan) Co., Ltd.

    China China
    Active

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