TAGORIZINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C30H36N4O
Molecular Weight	468.633
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC=C(\C=C\C(=O)NCCCCN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4)C=N1

InChI

InChIKey=DVYCNKDRINREMB-WUKNDPDISA-N

InChI=1S/C30H36N4O/c1-25-14-15-26(24-32-25)16-17-29(35)31-18-8-9-19-33-20-22-34(23-21-33)30(27-10-4-2-5-11-27)28-12-6-3-7-13-28/h2-7,10-17,24,30H,8-9,18-23H2,1H3,(H,31,35)/b17-16+

HIDE SMILES / InChI

Molecular Formula	C30H36N4O
Molecular Weight	468.633
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7916384 | https://www.ncbi.nlm.nih.gov/pubmed/7630045 | https://www.ncbi.nlm.nih.gov/pubmed/7780684

Tagorizine (also known as AL-3264) is a pyridylacrylamidoalkylpiperazine derivative patented by Dainippon Pharmaceutical Co., Ltd as an antiallergic agent. Tagorizine acts as 5-lipoxygenase inhibitor and blocks histamine H1-receptors in isolated guinea pig trachea, inhibits antigen-induced histamine release from isolated rat peritoneal mast cells, and suppress leukotriene production from activated human leukocytes. In preclinical models Tagorizine inhibited the antigen-induced leukotriene production in the abdominal cavity of passively sensitized rats and suppressed the arachidonic acid-induced ear edema in mice.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
smooth muscle contraction 13 Target ID: GO:0006939 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7780684	Inhibitor 8297
arachidonate 5-lipoxygenase activity 1 Target ID: GO:0004051 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7681286 \| https://adisinsight.springer.com/drugs/800002636	Inhibitor 8297	4.9 µM [IC50]
Histamine H1 receptor 315 Target ID: CHEMBL231 Sources: https://adisinsight.springer.com/drugs/800002636 \| https://www.ncbi.nlm.nih.gov/pubmed/7681286	Antagonist 2778

PubMed

Title	Date	PubMed
Inhibition of leukotriene production by N-[4-[4-(diphenylmethyl)-1- piperazinyl]butyl]-3-(6-methyl-3-pyridyl) acrylamide (AL-3264), a new antiallergic agent.	1994 May	7916384

Patents

Sample Use Guides

In Vivo Use Guide

rat 30 100 mg/kg

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:35:19 UTC 2023` Edited by `admin` on `Fri Dec 15 16:35:19 UTC 2023`
Record UNII	668QM8QJFS
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TAGORIZINE

Official Name

English

BROIZINE [JAN]

Common Name

English

AL-3264

Code

English

tagorizine [INN]

Common Name

English

AL3264

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C1322