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Tropisetron

Tropisetron structure

CAS No:
89565-68-4
Formula:
C17H20N2O2
Chemical Name:
Tropisetron
Synonyms:
1H-Indole-3-carboxylic acid,(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester;1H-Indole-3-carboxylic acid,8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester,endo-;Tropisetron;ICS 205930;Navoban;ICS 205-930;121061-97-0;2407912-00-7
Categories:
Active Pharmaceutical Ingredients > Digestive System Drugs

Description

ChEBI: An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine.

1H-indole-3-carboxylic acid (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) ester is an indolyl carboxylic acid.|An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.

Tropisetron Basic Attributes

Molecular Weight：

284.35

Exact Mass：

284.35

EC Number：

1806241-263-5

DSSTox ID：

DTXSID2044137

Characteristics

PSA：

45.3

XLogP3：

4.38640

Appearance：

white solid

Density：

1.26

Melting Point：

201-202 °C

Boiling Point：

448.5ºC at 760 mmHg

Flash Point：

225ºC

Refractive Index：

1.644

Water Solubility：

H2O: soluble

Storage Conditions：

2-8°C

Safety Information

wgk germany：

Drug Information

MeSH：

Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)|Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS. (See all compounds classified as Serotonin 5-HT3 Receptor Antagonists.)

MeSH Entry Terms：

(3 alpha-tropanyl)-1H-indole-3-carboxylic acid ester

Tropisetron Use and Manufacturing

Methods of Manufacturing

Tropinol (I) reacts with acid chloride (II) to get tropisetron.

Uses

Serotonin antagonist

Computed Properties

Molecular Weight:284.35
XLogP3:3.8
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:3
Exact Mass:284.152477885
Monoisotopic Mass:284.152477885
Topological Polar Surface Area:45.3
Heavy Atom Count:21
Complexity:400
Undefined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is a potent and highly selective competitive antagonist of 5-hydroxytryptamine 3 (5-HT3) receptors in peripheral neurons and the central nervous system. It inhibits the vomiting reflex by selectively blocking the presynaptic 5-HT3 receptors of peripheral neurons. It may also inhibit the stimulation of the vagus nerve in the rear region by directly blocking the central 5-HT3 receptors.

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

Tropisetron Hydrochloride Injection
Ingredients	Each ampoule of this drug contains 5.64 mg/5 mL of tropisetron hydrochloride, equivalent to 5 mg/5 mL of tropisetron.
Indication	1. If tropisetron hydrochloride is used simultaneously with rifampicin or other liver enzyme inducing drugs (such as phenobarbital), the plasma concentration of tropisetron hydrochloride may be reduced, so patients with normal metabolism need to increase the dose (patients with poor metabolizers do not need to increase the dose). 2. Cytochrome P450 enzyme inhibitors such as cimetidine have little effect on the plasma concentration of tropisetron hydrochloride, and no dose adjustment is required under normal use.
Specifications	5ml:5mg
Manufacturer	KP Pharmacy Co., Ltd.

Tropisetron Hydrochloride Injection
Ingredients	Each ampoule of this drug contains 5.64 mg/5 mL of tropisetron hydrochloride, equivalent to 5 mg/5 mL of tropisetron.
Indication	1. If tropisetron hydrochloride is used simultaneously with rifampicin or other liver enzyme inducing drugs (such as phenobarbital), the plasma concentration of tropisetron hydrochloride may be reduced, so patients with normal metabolism need to increase the dose (patients with poor metabolizers do not need to increase the dose). 2. Cytochrome P450 enzyme inhibitors such as cimetidine have little effect on the plasma concentration of tropisetron hydrochloride, and no dose adjustment is required under normal use.
Specifications	5ml:5mg
Manufacturer	Shanxi PUDE Pharmaceutical Co., Ltd.

Tropisetron Hydrochloride Injection
Ingredients	Each ampoule of this drug contains 5.64 mg/5 mL of tropisetron hydrochloride, equivalent to 5 mg/5 mL of tropisetron.
Indication	1. If tropisetron hydrochloride is used simultaneously with rifampicin or other liver enzyme inducing drugs (such as phenobarbital), the plasma concentration of tropisetron hydrochloride may be reduced, so patients with normal metabolism need to increase the dose (patients with poor metabolizers do not need to increase the dose). 2. Cytochrome P450 enzyme inhibitors such as cimetidine have little effect on the plasma concentration of tropisetron hydrochloride, and no dose adjustment is required under normal use.
Specifications	5ml:5mg
Manufacturer	Qinghai Chenfei Pharmaceutical Co., Ltd.

See More Related Drugs

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