TROPANSERIN

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H23NO2
Molecular Weight	273.37
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CN1[C@H]2CC[C@@H]1C[C@@H](C2)OC(=O)C3=CC(C)=CC(C)=C3

InChI

InChIKey=HDDNYFLPWFSBLN-ZSHCYNCHSA-N

InChI=1S/C17H23NO2/c1-11-6-12(2)8-13(7-11)17(19)20-16-9-14-4-5-15(10-16)18(14)3/h6-8,14-16H,4-5,9-10H2,1-3H3/t14-,15+,16+

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Description

Tropanserin (MDL 72422) is a potent and selective 5-HT3 receptor antagonist. It was investigated as a drug for the treatment of migraine. MDL 72222 was shown to be an effective antimigraine agent in a double-blind placebo-controlled study.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 3 (5-HT3) receptor	Antagonist

Conditions

Condition	Modality	Targets	Highest Phase	Product
Migraine	Primary		Phase II	Unknown

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
ChemBridge	5254007	http://www.hit2lead.com/screening-compounds/5254007
ChemDiv	4480-0919	http://chemistryondemand.com:8080/eShop/search_results.jsp?idnumber=4480-0919
eMolecules	1304629	https://orderbb.emolecules.com/search/#?query=1304629
eMolecules	33422852	https://orderbb.emolecules.com/search/#?query=33422852
Lab Network	LN01043686	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01043686

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PubMed

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Title	Date	PubMed
5HT2 and 5HT3 receptors' contribution to modeling of post-serotonin respiratory pattern in cats.	2004 Sep 24	15350826
GABA(A) receptors mediate the attenuating effects of a 5-HT(3) receptor antagonist on methamphetamine-induced behavioral sensitization in mice.	2010 Apr	19953653
Analgesia induced by 2- or 100-Hz electroacupuncture in the rat tail-flick test depends on the anterior pretectal nucleus.	2013 Nov 6	24063986

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Patents

Sample Use Guides

In Vivo Use Guide

Forty-seven patients with common (n = 29) or classical (n = 8) migraine or mixed type with or without a psychogenic component (n = 10) received 20-40 mg Tropanserin (MDL-72,422) (n = 24) or placebo (n = 23) intravenously during the headache phase of a migraine attack.

Route of Administration: Intravenous

In Vitro Use Guide

Treatment of rat ganglia with the 5-HT(3) receptor antagonist Tropanserin (MDL 72222) (0.5 uM) during the maintenance phase of established gLTD (1 h after LFS) antagonized the LFS-induced depression.

Show entries

Name

Type

Language

TROPANSERIN

Official Name

English

BENZOIC ACID, 3,5-DIMETHYL-, (3-ENDO)-8-METHYL-8-AZABICYCLO(3.2.1)OCT-3-YL ESTER

Common Name

English

tropanserin [INN]

Common Name

English

BENZOIC ACID, 3,5-DIMETHYL-, 8-METHYL-8-AZABICYCLO(3.2.1)OCT-3-YL ESTER, ENDO-

Common Name

English

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Classification Tree

Code System

Code

Agent Affecting Nervous System

NCI_THESAURUS

C66885

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Code System

Code

Type

Description

EPA CompTox

DTXSID0042618

PRIMARY

CHEBI

64142

PRIMARY

CAS

85181-40-4

PRIMARY

ChEMBL

CHEMBL1742402

PRIMARY

EVMPD

SUB11338MIG

PRIMARY

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ACTIVE MOIETY


					04B48I6VHR

TROPANSERIN