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 |
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Proceedings: Antihypertensive activity of a new 3-hydrazinopyridazine derivative: ISF 2123. | 1974 Nov |
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[Effect of a new derivative of 3-hydrazine pyridazine: ISF 2123 in hypertensive patients. Note 2]. | 1975 Dec |
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[Activity of a new derivative of 3-hydrazinopyridazine: ISF 2123 in patients with hypertension. I]. | 1975 Nov |
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A new antihypertensive compound: 3 hydrazino-6- [(2-hydroxypropyl)methylamino] pyridazine dihydrochloride (ISF 2123). | 1976 Jun |
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[Clinical pharmacology of a new hypotensive drug with peripheral vasodilating action (ISF 2123); effects of acute intravenous administration in hypertensive patients]. | 1977 |
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Characteristics and clinical effects of ISF 2123, a new antihypertensive agent. | 1977 Jan |
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[Derivatives of 3-hydrazinopyridazine. II. Synthesis and antihypertensive activity of new 3-hydrazino-6-monoalkylaminopyridazines]. | 1978 Feb |
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Mechanism of action of hydralazine and ISF 2123 on arterial smooth muscle [proceedings]. | 1978 Mar |
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Quantitative determination of propildazine in rat plasma by gas-liquid chromatography. | 1978 Nov 21 |
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[Treatment of severe arterial hypertension with propyldazine (ISF 2123) associated with a diuretic and a beta-blocking agent]. | 1979 Mar |
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Carcinogenicity study in mice on pildralazine, a hydralazinelike antihypertensive compound. | 1983 |
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Effects of pildralazine alone and in combination on severe hypertension and cerebrovascular lesions in saline-drinking spontaneously hypertensive rats. | 1984 |
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Kinetic studies of the tissue binding tendency of the new vasodilator pildralazine. | 1987 Apr |
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
by
admin
on
Edited
Fri Dec 15 16:05:45 GMT 2023
by
admin
on
Fri Dec 15 16:05:45 GMT 2023
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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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C009978
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Pildralazine
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