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
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)
| Molecular Formula | C8H15N5O |
| Molecular Weight | 197.2376 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
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
| Title | Date | PubMed |
|---|---|---|
| Kinetic studies of the tissue binding tendency of the new vasodilator pildralazine. | 1987-04 |
|
| Effects of pildralazine alone and in combination on severe hypertension and cerebrovascular lesions in saline-drinking spontaneously hypertensive rats. | 1984 |
|
| Carcinogenicity study in mice on pildralazine, a hydralazinelike antihypertensive compound. | 1983 |
|
| [Treatment of severe arterial hypertension with propyldazine (ISF 2123) associated with a diuretic and a beta-blocking agent]. | 1979-03 |
|
| Quantitative determination of propildazine in rat plasma by gas-liquid chromatography. | 1978-11-21 |
|
| Mechanism of action of hydralazine and ISF 2123 on arterial smooth muscle [proceedings]. | 1978-03 |
|
| [Derivatives of 3-hydrazinopyridazine. II. Synthesis and antihypertensive activity of new 3-hydrazino-6-monoalkylaminopyridazines]. | 1978-02 |
|
| Characteristics and clinical effects of ISF 2123, a new antihypertensive agent. | 1977-01 |
|
| [Clinical pharmacology of a new hypotensive drug with peripheral vasodilating action (ISF 2123); effects of acute intravenous administration in hypertensive patients]. | 1977 |
|
| A new antihypertensive compound: 3 hydrazino-6- [(2-hydroxypropyl)methylamino] pyridazine dihydrochloride (ISF 2123). | 1976-06 |
|
| [Effect of a new derivative of 3-hydrazine pyridazine: ISF 2123 in hypertensive patients. Note 2]. | 1975-12 |
|
| [Activity of a new derivative of 3-hydrazinopyridazine: ISF 2123 in patients with hypertension. I]. | 1975-11 |
|
| Proceedings: Antihypertensive activity of a new 3-hydrazinopyridazine derivative: ISF 2123. | 1974-11 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6541924
Curator's Comment: Rats data
Single dose - 1 mg/kg for 13 weeks
Route of Administration:
Oral
| Substance Class |
Chemical
Created
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admin
on
Edited
Mon Mar 31 18:18:48 GMT 2025
by
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Mon Mar 31 18:18:48 GMT 2025
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| Record UNII |
FU2BGC781U
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| Record Status |
Validated (UNII)
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| Record Version |
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NCI_THESAURUS |
C29707
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m8805
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CHEMBL2107172
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FU2BGC781U
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C009978
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Pildralazine
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SUB09833MIG
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