TRAPIDIL

Details

Stereochemistry	ACHIRAL
Molecular Formula	C10H15N5
Molecular Weight	205.2596
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCN(CC)C1=CC(C)=NC2=NC=NN12

InChI

InChIKey=GSNOZLZNQMLSKJ-UHFFFAOYSA-N

InChI=1S/C10H15N5/c1-4-14(5-2)9-6-8(3)13-10-11-7-12-15(9)10/h6-7H,4-5H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C10H15N5
Molecular Weight	205.2596
Charge	0
Count

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

Description
Sources: http://www.drugbank.ca/drugs/DB09283
Curator's Comment: Description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/19110816

Trapidil, a platelet-derived growth factor antagonist, was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease. Used to treat patients with ischemic coronary heart, liver, and kidney disease.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Thrombin-induced Thromboxane formation 1 Target ID: Thrombin-induced Thromboxane formation Sources: http://www.ncbi.nlm.nih.gov/pubmed/3248101	Inhibitor 8297	410.0 µM [IC50]
Platelet-derived growth factor receptor beta 56 Target ID: CHEMBL1913 Sources: http://www.ncbi.nlm.nih.gov/pubmed/7861694	Antagonist 2778
C-C motif chemokine 2 2 Target ID: P28292 Gene ID: 1.00009128E8 Gene Symbol: CCL2 Target Organism: Oryctolagus cuniculus (Rabbit) Sources: http://www.ncbi.nlm.nih.gov/pubmed/10576207	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Coronary heart disease 41 Sources: http://memim.com/trapidil.html	Primary		Approved 8429	Trapidil Approved Use Trapidil is primarily used for the treatment of coronary heart disease (CHD ) by reducing the preload and afterload of the heart muscle, especially in patients with an intolerance to the standard used ingredients from the class of nitrates. In addition, it decreases after a myocardial infarction, the incidence of other cardiovascular complications. In patients with peripheral arterial occlusive disease Trapidil improves blood flow to the limbs and walking performance. Launch Date 2000

PubMed

Title	Date	PubMed
Osteitis fibrosa is mediated by Platelet-Derived Growth Factor-A via a phosphoinositide 3-kinase-dependent signaling pathway in a rat model for chronic hyperparathyroidism.	2008 Nov	18635661

Patents

Sample Use Guides

In Vivo Use Guide

Adults: Oral: 400-600 mg/day in divided doses

Route of Administration: Oral

In Vitro Use Guide

The addition of 100 to 400 ug/ml Trapidil significantly reduced cell proliferation induced by different growth factors (FCS, PDGF-BB, bFGF, EGF)

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:48:51 GMT 2023` Edited by `admin` on `Fri Dec 15 15:48:51 GMT 2023`
Record UNII	EYG5Y6355E
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TRAPIDIL

Official Name

English

TRAPIDIL [MI]

Common Name

English

Trapidil [WHO-DD]

Common Name

English

AR 12008

Code

English

ROCORNAL

Brand Name

English

TRAPIDIL [JAN]

Common Name

English

TRAPIDIL [MART.]

Common Name

English

trapidil [INN]

Common Name

English

AR-12008

Code

English

TRAPIDIL [EP MONOGRAPH]

Common Name

English

7-(DIETHYLAMINO)-5-METHYL-S-TRIAZOLO(1,5-A)PYRIMIDINE.

Systematic Name

English

Classification Tree Code System Code

WHO-VATC

QC01DX11