FABESETRON HYDROCHLORIDE

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C18H19N3O.ClH
Molecular Weight	329.824
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

Cl.CC1=C(C[C@H]2CCC3=C(C)C4=C(C=CC=C4)N3C2=O)N=CN1

InChI

InChIKey=POKFYJWUPWZYQV-BTQNPOSSSA-N

InChI=1S/C18H19N3O.ClH/c1-11-14-5-3-4-6-17(14)21-16(11)8-7-13(18(21)22)9-15-12(2)19-10-20-15;/h3-6,10,13H,7-9H2,1-2H3,(H,19,20);1H/t13-;/m1./s1

HIDE SMILES / InChI

Description

Fabesetron is a dual 5HT3 and 5HT4 receptors antagonist that was developed in Japan for the treatment of chemotherapy-induced emesis and gastrointestinal disorders. The development of the drug was terminated in phase II.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
5-hydroxytryptamine receptor 4 8	Antagonist 2,849
5-hydroxytryptamine receptor 3A 7	Antagonist 2,849		8.84 null [pIC50]

Conditions

Condition	Modality	Highest Phase	Product
Vomiting 38	Secondary	Phase II 1,147	Unknown
Gastrointestinal disorders 94	Primary	Phase II 1,147	Unknown
Nausea 63	Secondary	Phase II 1,147	Unknown

PubMed

Show entries

Title	Date	PubMed
Effect of FK1052, a potent 5-hydroxytryptamine3 and 5-hydroxytryptamine4 receptor dual antagonist, on colonic function in vivo.	1993 Jul	8331576
New 5-HT3 (serotonin-3) receptor antagonists, II. Synthesis and structure-activity relationships of pyrimido[1,6-a]indoles.	1994 Dec	7697772
Combined blockade of 5-HT3- and 5-HT4-serotonin receptors inhibits colonic functions in conscious rats and mice.	1997 Apr	9103508

Showing 1 to 3 of 3 entries

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Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Unknown

In Vitro Use Guide

The effect of fabesteron on short-circuit current was investigated using submucosa-mucosa sheets of guinea-pig distal colon. The drug at 10(-9) M suppressed the 5-HT-evoked response to 69% of control.

Show entries

Name

Type

Language

FABESETRON HYDROCHLORIDE

Common Name

English

FK-1052

Preferred Name

English

PYRIDO(1,2-A)INDOL-6(7H)-ONE, 8,9-DIHYDRO-10-METHYL-7-((5-METHYL-1H-IMIDAZOL-4-YL)METHYL)-, MONOHYDROCHLORIDE, (R)-

Common Name

English

FABESETRON HYDROCHLORIDE [JAN]

Common Name

English

PYRIDO(1,2-A)INDOL-6(7H)-ONE, 8,9-DIHYDRO-10-METHYL-7-((5-METHYL-1H-IMIDAZOL-4-YL)METHYL)-, MONOHYDROCHLORIDE, (7R)-

Common Name

English

Showing 1 to 5 of 7 entries

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Show entries

Code System

Code

Type

Description

CHEBI

31588

PRIMARY

FDA UNII

DIU098C1O7

PRIMARY

EPA CompTox

DTXSID7048168

PRIMARY

PUBCHEM

180494

PRIMARY

CAS

129299-90-7

PRIMARY

Showing 1 to 5 of 5 entries

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ACTIVE MOIETY


					QU72HVX338

FABESETRON

SUBSTANCE RECORD


					DIU098C1O7

FABESETRON HYDROCHLORIDE