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Details

Stereochemistry ACHIRAL
Molecular Formula C9H9Cl2N3O
Molecular Weight 246.093
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GUANFACINE

SMILES

NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl

InChI

InChIKey=INJOMKTZOLKMBF-UHFFFAOYSA-N
InChI=1S/C9H9Cl2N3O/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13/h1-3H,4H2,(H4,12,13,14,15)

HIDE SMILES / InChI

Molecular Formula C9H9Cl2N3O
Molecular Weight 246.093
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

Etiguanfacine, also known as SSP-1871, is an α2-adrenoreceptor agonist.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
7.03 null [pKi]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TENEX
Primary
TENEX

Cmax

ValueDoseCo-administeredAnalytePopulation
7 ng/mL
4 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens
10 ng/mL
4 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens
2.5 ng/mL
1 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
116 ng × h/mL
4 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens
162 ng × h/mL
4 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens
56 ng × h/mL
1 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
16 h
1 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
30%
1 mg 1 times / day multiple, oral
GUANFACINE plasma
Homo sapiens

Doses

AEs

Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Usual Adult Dose for Hypertension Initial dose: 1 mg orally once a day at bedtime; may increase to 2 mg once a day if satisfactory result not achieved after 3 to 4 weeks. Usual Pediatric Dose for Attention Deficit Disorder 6 YEARS TO LESS THAN 18 YEARS: Initial dose: 1 mg orally once a day, either in the morning or evening, at approximately the same time each day; may adjust in increments of no more than 1 mg/week. Recommended target dose: 0.05 to 0.12 mg/kg/day (total daily dose between 1 and 7 mg) once a day, depending on clinical response and tolerability Maximum dose: 6 to 12 years: Doses above 4 mg/day have not been evaluated; 13 to 17 years: Doses above 7 mg/day have not been evaluated.
Route of Administration: Oral
In Vitro Use Guide
Guanfacine and clonidine at relatively high concentrations (10(-6)-10(-4) M) produced contractions of the rat vas deferens which were antagonized by prazosin.
Substance Class Chemical
Record UNII
30OMY4G3MK
Record Status Validated (UNII)
Record Version