U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry RACEMIC
Molecular Formula C8H15N5O
Molecular Weight 197.2376
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PILDRALAZINE

SMILES

CC(O)CN(C)C1=NN=C(NN)C=C1

InChI

InChIKey=KYIAWOXNPBANEW-UHFFFAOYSA-N
InChI=1S/C8H15N5O/c1-6(14)5-13(2)8-4-3-7(10-9)11-12-8/h3-4,6,14H,5,9H2,1-2H3,(H,10,11)

HIDE SMILES / InChI

Molecular Formula C8H15N5O
Molecular Weight 197.2376
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Pildralazine is a hydralazinelike antihypertensive vasodilator containing a free hydrazine group. Potency of the compound was shown to be from 6 to 10 times greater than that of hydralazine although, from a qualitative point of view, the two drugs act similarly. Pildralazine was shown to be inactive on nictitating membrane contractions induced by sympathetic stimulation or by adrenaline injection into the lingual artery. However, it antagonized the vascular effects of adrenaline, angiotensin and vasopressin in pithed rats and spinal cats. Pildralazine significantly inhibited the onset of severe hypertension in rats; the combination of pildralazine with moderately effective doses of propranolol or dihydrochlorothiazide completely prevented the blood pressure increase. Whereas a lack of carcinogenic activity has been reported for pildralazine in 1983, a report published in Germany in 1985 states the drug to be mutagenic with auxotrophic mutants of S.Typhimurium and E.coli.

Originator

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
Single dose - 1 mg/kg for 13 weeks
Route of Administration: Oral
Substance Class Chemical
Record UNII
FU2BGC781U
Record Status Validated (UNII)
Record Version