FABESETRON

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C18H19N3O
Molecular Weight	293.363
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

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

InChI

InChIKey=AEKQMJRJRAHOAP-CYBMUJFWSA-N

InChI=1S/C18H19N3O/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)/t13-/m1/s1

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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
New 5-HT3 (serotonin-3) receptor antagonists, II. Synthesis and structure-activity relationships of pyrimido[1,6-a]indoles.	1994 Dec	7697772
New 5-HT3 (serotonin-3) receptor antagonists. III. An efficient synthesis of carbon 14-labeled (+)-8,9-dihydro-10-methyl-7-[(5-methyl-1H-imidazol-4- yl)methyl]pyrido[1,2-a]indol-6(7H)-one hydrochloride (FK 1052).	1995 Aug	7553979
Probable involvement of the 5-hydroxytryptamine(4) receptor in methotrexate-induced delayed emesis in dogs.	2000 Mar	10688616

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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 [INN]

Preferred Name

English

FABESETRON

Official Name

English

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

Systematic Name

English

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Show entries

Classification Tree

Code System

Code

Serotonin Antagonist

NCI_THESAURUS

C94726

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Code System

Code

Type

Description

EPA CompTox

DTXSID2048169

PRIMARY

CAS

129300-27-2

PRIMARY

FDA UNII

QU72HVX338

PRIMARY

EVMPD

SUB07496MIG

PRIMARY

SMS_ID

100000081531

PRIMARY

Showing 1 to 5 of 10 entries

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ACTIVE MOIETY


					QU72HVX338

FABESETRON

SALT/SOLVATE (PARENT)


					DIU098C1O7

FABESETRON HYDROCHLORIDE