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Details

Stereochemistry ACHIRAL
Molecular Formula C10H13N3
Molecular Weight 175.2303
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DEBRISOQUIN

SMILES

NC(=N)N1CCC2=C(C1)C=CC=C2

InChI

InChIKey=JWPGJSVJDAJRLW-UHFFFAOYSA-N
InChI=1S/C10H13N3/c11-10(12)13-6-5-8-3-1-2-4-9(8)7-13/h1-4H,5-7H2,(H3,11,12)

HIDE SMILES / InChI

Description

Debrisoquin is an antihypertensive drug having guanethidine-like properties, which inhibits monoamine oxidase (MAO) and does not enter the brain. Debrisoquine was used for the treatment of hypertension. Debrisoquine hydroxylation phenotype has been the most used test in humans to evaluate CYP2D6 activity. Two debrisoquine hydroxylation phenotypes have been described: poor and extensive metabolizers. A group with a very low debrisoquine metabolic ratio within the extensive metabolizers, named ultrarapid metabolizers, has also been distinguished. This CYP2D6 variability can be for a large part alternatively determined by genotyping, which appears to be of clinical importance given CYP2D6 involvement in the metabolism of a large number of commonly prescribed drugs.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.5 µM [IC50]
8.8 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
DECLINAX

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Adult: 10-20 mg once-bid, increased by 10-20 mg every 3 or 4 days according to severity of condition. Maintenance: 20-120 mg daily. Max Dosage: ≥300 mg daily. More: https://www.ndrugs.com/?s=declinax
Route of Administration: Oral
In Vitro Use Guide
Unknown