PIBAXIZINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H29NO4
Molecular Weight	395.4914
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)COCCOCCN1CCC(CC1)=C(C2=CC=CC=C2)C3=CC=CC=C3

InChI

InChIKey=KMUBBNQZNBTUSH-UHFFFAOYSA-N

InChI=1S/C24H29NO4/c26-23(27)19-29-18-17-28-16-15-25-13-11-22(12-14-25)24(20-7-3-1-4-8-20)21-9-5-2-6-10-21/h1-10H,11-19H2,(H,26,27)

HIDE SMILES / InChI

Description
Sources: https://adisinsight.springer.com/drugs/800003720 | https://www.ncbi.nlm.nih.gov/pubmed/3899673 | DOI: 10.1002/0471238961.0809192010011419.a01 | https://apps.who.int/iris/bitstream/handle/10665/67830/WHO_EDM_QSM_2003.2.pdf

Pibaxizine is diphenylmethyl piperazine derivatives. It is a histamine H1 receptor antagonist. Animal experiments have shown that it has spasmolytic properties for smooth muscle, particularly in the bronchi, as well as anticholinergic and anti-serotonin activities. It can be concluded that Pibaxizine has a strong protective effect against bronchospasm caused by inhalation of a histamine aerosol. Protection against methacholine-induced bronchospasm was less marked. Pibaxizine had been in phase II clinical trial for the treatment of chronic obstructive pulmonary disease. However, this development was discontinued.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
smooth muscle contraction 13 Target ID: GO:0006939 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3899673	Inhibitor 8504

PubMed

Title	Date	PubMed
Protective effect by UCB JO28 against histamine and methacholine induced bronchial hyperreactivity.	1985	3899673

Name

Type

Language

pibaxizine [INN]

Preferred Name

English

PIBAXIZINE

Official Name

English

(2-(2-(4-(DIPHENYLMETHYLENE)PIPERIDINO)ETHOXY)ETHOXY)ACETIC ACID

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29578