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Details

Stereochemistry ACHIRAL
Molecular Formula C8H8N4
Molecular Weight 160.1759
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of HYDRALAZINE

SMILES

NNC1=NN=CC2=C1C=CC=C2

InChI

InChIKey=RPTUSVTUFVMDQK-UHFFFAOYSA-N
InChI=1S/C8H8N4/c9-11-8-7-4-2-1-3-6(7)5-10-12-8/h1-5H,9H2,(H,11,12)

HIDE SMILES / InChI

Molecular Formula C8H8N4
Molecular Weight 160.1759
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Hydralazine is a direct-acting vasodilator that is used as an antihypertensive agent. Hydralazine works by relaxing blood vessels (arterioles more than venules) and increasing the supply of blood and oxygen to the heart while reducing its workload. It also functions as an antioxidant. It inhibits membrane-bound enzymes that form reactive oxygen species, such as superoxides. Excessive superoxide counteracts NO-induced vasodilation. Hydralazine is used for the treatment of essential hypertension, alone or as an adjunct. Also for the management of severe hypertension when the drug cannot be given orally or when blood pressure must be lowered immediately, congestive heart failure (in combination with cardiac glycosides and diuretics and/or with isosorbide dinitrate), and hypertension secondary to pre-eclampsia/eclampsia.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
400.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Hydralazine Hydrochloride

Cmax

ValueDoseCo-administeredAnalytePopulation
3 μM
50 mg single, oral
HYDRALAZINE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
407 μM × h
50 mg single, oral
HYDRALAZINE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
2 h
50 mg single, oral
HYDRALAZINE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
13%
HYDRALAZINE plasma
Homo sapiens

Doses

AEs

Drug as perpetrator​

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Initial dose: 10 mg orally 4 times a day for the first 2 to 4 days. Increase to 25 mg orally 4 times a day for the balance of the first week. For the second and subsequent weeks, increase dosage to 50 mg orally 4 times a day.
Route of Administration: Oral
In Vitro Use Guide
Hydralazine (0.03-10 mmol.L(-1)) inhibited the activities of both PKA and PKG with IC50 of 1.2 and 2.5 mmol.L(-1), respectively
Substance Class Chemical
Record UNII
26NAK24LS8
Record Status Validated (UNII)
Record Version