TODRALAZINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C11H12N4O2
Molecular Weight	232.2386
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC(=O)NNC1=C2C=CC=CC2=CN=N1

InChI

InChIKey=WGZDBVOTUVNQFP-UHFFFAOYSA-N

InChI=1S/C11H12N4O2/c1-2-17-11(16)15-14-10-9-6-4-3-5-8(9)7-12-13-10/h3-7H,2H2,1H3,(H,13,14)(H,15,16)

HIDE SMILES / InChI

Molecular Formula	C11H12N4O2
Molecular Weight	232.2386
Charge	0
Count

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

Description
Sources: www.drugfuture.com/mt/tocoferil-nicotinate.pdf
Curator's Comment: description was created based on several sources, including: http://www.ncbi.nlm.nih.gov/pubmed/6425526 http://www.naoru.com/Apiracohl.html http://www.ncbi.nlm.nih.gov/pubmed/9412993

Todralazine is a hydralazinophthalazine-derived drug currently used in the treatment of arterial hypertension. As vasodilator, it might be used in combination with isosorbide dinitrate. Side effects and drug toxicity were uncommon in such vasodilator therapy.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Collagenase 5 Target ID: CHEMBL2095216 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2169725	Activator 1430
histone acetylation 5 Target ID: GO:0016573 Sources: http://www.ncbi.nlm.nih.gov/pubmed/17156885	Inhibitor 8297
Lysosomal alpha-glucosidase 9 Target ID: CHEMBL2608 Sources: http://www.ncbi.nlm.nih.gov/pubmed/3266791	Activator 1430

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 567 Sources: http://www.jp-orangebook.gr.jp/cgi-bin/search_h/search_e.cgi?action=detail_frame&effect=214%20&find=Todralazine%20Hydrochloride%20Hydrate	Primary		Approved 8429	Unknown Approved Use Todralazine is used as an antihypertensive agent

PubMed

Title	Date	PubMed
[The influence of guanazodine and todralazine on blood pressure regulation during dynamic and static exercise in essential hypertension (author's transl)].	1977	580022

Patents

Sample Use Guides

In Vivo Use Guide

40 – 120 mg in 3 doses per day

Route of Administration: Oral

In Vitro Use Guide

Todralazine (TDR) decreased the free radical level in granulocyte samples. At the highest of the tested TDR concentrations (80 μg/ml), the free radical level was lower by ~40% in the samples where only TDR was present than in the control samples (spontaneous release, without TDR).

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:54:56 GMT 2023` Edited by `admin` on `Fri Dec 15 15:54:56 GMT 2023`
Record UNII	WEN3K83YKD
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TODRALAZINE

Official Name

English

NSC-757868

Code

English

Todralazine [WHO-DD]

Common Name

English

CEPH

Code

English

todralazine [INN]

Common Name

English

ETHYL 3-(1-PHTHALAZINYL)CARBAZATE

Systematic Name

English

BT-621 FREE BASE

Code

English

TODRALAZINE [MI]

Common Name

English

CEPH FREE BASE

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C29707