GUANFACINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C9H9Cl2N3O
Molecular Weight	246.0935
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

c1cc(c(CC(=NC(=N)N)O)c(c1)Cl)Cl

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	246.0935
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019032s021lbl.pdf | https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf

Guanfacine (marketed under the brand names Estulic, Tenex and the extended release Intuniv) is a sympatholytic drug, indicated for the management of hypertension. Tenex (guanfacine hydrochloride) is an orally active antihypertensive agent whose principal mechanism of action appears to be stimulation of central α2-adrenergic receptors. By stimulating these receptors, guanfacine reduces sympathetic nerve impulses from the vasomotor center to the heart and blood vessels. This results in a decrease in peripheral vascular resistance and a reduction in heart rate. Guanfacine is also used in the treatment of attention deficit hyperactivity disorder. Intuniv is an extended-release version of guanfacine that is used to treat symptoms of ADHD. It can be used by itself or with stimulant medications also used to treat symptoms of ADHD.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Alpha-2a adrenergic receptor 62 Target ID: CHEMBL1867 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019032s021lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/9605427	Agonist 2470		7.03 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019032s021lbl.pdf	Primary		Approved 8043	TENEX Approved Use Tenex (guanfacine hydrochloride) is indicated in the management of hypertension. Tenex may be given alone or in combination with other antihypertensive agents, especially thiazide-type diuretics. Launch Date 5.30755191E11
Attention deficit hyperactivity disorder 62 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	Primary		Approved 8043	TENEX Approved Use INTUNIV® is a central alpha2A-adrenergic receptor agonist indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) as monotherapy and as adjunctive therapy to stimulant medications Launch Date 5.30755191E11

C_max

Value	Dose	Analyte	Population
7 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: ADOLESCENT sex: UNKNOWN food status: UNKNOWN
10 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: CHILD sex: UNKNOWN food status: UNKNOWN
2.5 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
116 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: ADOLESCENT sex: UNKNOWN food status: UNKNOWN
162 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: CHILD sex: UNKNOWN food status: UNKNOWN
56 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
16 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:		GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
30% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:		GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
12 mg single, oral Overdose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/	unhealthy, 12 years n = 1 Health Status: unhealthy Condition: ADHD and Tourette syndrome Age Group: 12 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/	Disc. AE: Hypertensive... AEs leading to discontinuation/dose reduction: Hypertensive (1%) Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/	unhealthy, 17 years n = 1 Health Status: unhealthy Condition: ADHD Age Group: 17 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/	Disc. AE: Cardiogenic pulmonary edema... AEs leading to discontinuation/dose reduction: Cardiogenic pulmonary edema (1%) Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/
4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (6%) Fatigue (2%) Hypotension (1%) Headache (1%) Dizziness (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	unhealthy, children n = 16 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Age Group: children Population Size: 16 Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	Other AEs: Sedation, Fatigue... Other AEs: Sedation (below serious, 5 patients) Fatigue (below serious, 3 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT01069523

AEs

AE	Significance	Dose	Population
Hypertensive	1% Disc. AE	12 mg single, oral Overdose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/	unhealthy, 12 years n = 1 Health Status: unhealthy Condition: ADHD and Tourette syndrome Age Group: 12 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/
Cardiogenic pulmonary edema	1% Disc. AE	80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/	unhealthy, 17 years n = 1 Health Status: unhealthy Condition: ADHD Age Group: 17 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/
Dizziness	1% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Headache	1% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Hypotension	1% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Fatigue	2% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Somnolence	6% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Fatigue	below serious, 3 patients	4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	unhealthy, children n = 16 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Age Group: children Population Size: 16 Sources: https://clinicaltrials.gov/ct2/show/NCT01069523
Sedation	below serious, 5 patients	4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	unhealthy, children n = 16 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Age Group: children Population Size: 16 Sources: https://clinicaltrials.gov/ct2/show/NCT01069523

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1601	inhibitor 1604	inhibitor 1702	inhibitor 1475

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1383 CYP2C8 818 CYP2C19 1325 CYP3A4/5 241 CYP2B6 717	CYP3A4/5 76 P-gp 1400	CYP3A 118 CYP1A2 637 CYP2B6 501

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1532	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP1A2 1532	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2B6 884	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP2B6 884	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP2C19 1392	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2C8 865	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2C9 1648	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2D6 1738	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP3A 271	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP3A4/5 293	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1601	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0	major	yes (co-administration study) Comment: There was a significant decrease in the rate and extent of guanfacine exposure when co-administered with rifampin, a CYP3A4 inducer. The exposure to guanfacine decreased by 70% (AUC) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0
P-gp 1400	substrate 3113 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3173033/ Page: 18.0	weak
CYP3A4/5 76	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0	yes	yes (co-administration study) Comment: There was a substantial increase in the rate and extent of guanfacine exposure when administered with ketoconazole; the guanfacine exposure increased 3-fold (AUC) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1507	inhibitor 1489 Sources: https://www.tga.gov.au/sites/default/files/auspar-guanfacine-180503.pdf#page=30

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY546722	https://www.001chemical.com/chem/29110-47-2
AHH Chemical co.,ltd	MR-1013815	http://www.ahhchemical.com/product/MR-1013815.html
Alsachim	928	http://www.alsachim.com/product-C1246-glo.bal-view.html
Ambinter	Amb10843802	http://www.ambinter.com/reference/10843802
Angel Pharmatech	AG302778	http://www.angelpharmatech.com/29110-47-2.html
Angene	AGN-PC-04XZ20	http://www.angenechemical.com/productshow/AGN-PC-04XZ20.html
BLD Pharm	BD132435	http://www.bldpharm.com/products/29110-47-2.html
BioChemPartner	BCP09647	http://www.biochempartner.com/29110-47-2-BCP09647
BioCrick	BCC5180	http://www.biocrick.com/Guanfacine-BCC5180.html
BioSynth	J-017394	https://www.biosynth.com/en/products/all-products/products/J-017394.html
CSNpharm	CSN11127	https://www.csnpharm.com/products/guanfacine.html
Chem Scene	CS-2787	http://www.chemscene.com/29110-47-2.html
Clearsynth	CS-T-25721	https://www.clearsynth.com/en/CST25721.html
DC Chemicals	DC23226	http://www.dcchemicals.com/product_show-DC23226.html
Finetech	FT-0669068	http://www.finetechnology-ind.com/prod/detail/pub/1189924-28-4.html
Finetech	FT-0669067	http://www.finetechnology-ind.com/prod/detail/pub/29110-47-2.html
Hairui	HR141314	http://www.hairuichem.com/en/product/29110-47-2.html
Lab Network	LN01308386	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01308386
MedChem Express	HY-17416A	https://www.medchemexpress.com/guanfacine.html
Molcore	MC546722	https://www.molcore.com/product/29110-47-2
MuseChem	I003012	https://www.musechem.com/product/I003012.html
Smolecule	S576275	https://www.smolecule.com/products/s576275
Smolecule	S905071	https://www.smolecule.com/products/s905071
THE BioTek	bt-305246	https://www.thebiotek.com/product/others/bt-305246
Yuhao Chemical	RT3442	http://www.chemyuhao.com/29110-47-2.html

PubMed

Title	Date	PubMed
Bradycardia during epidural anesthesia in a patient receiving guanfacine.	1992 Dec	1466475
Centrally acting imidazoline I1-receptor agonists: do they have a place in the management of hypertension?	2001	14728014
Effects of alpha-adrenoceptor agonists in chronic morphine administered DSP4-treated rats: evidence for functional cross-sensitization.	2001 Oct	14715456
Why have drug treatments been so disappointing?	2003	14521196
Hallucinations associated with initiation of guanfacine.	2003 Dec	14627872
Growth hormone response to guanfacine in boys with attention deficit hyperactivity disorder: a preliminary study.	2003 Fall	14642016
The alpha2-adrenergic agonist guanfacine reduces excitability of human motor cortex through disfacilitation and increase of inhibition.	2003 Oct	14499745
Pharmacotherapy of pervasive developmental disorders in children and adolescents.	2004	15584771
The anticonvulsant and proconvulsant effects of alpha2-adrenoreceptor agonists are mediated by distinct populations of alpha2A-adrenoreceptors.	2004	15183527
alpha2a adrenoceptors regulate phosphorylation of microtubule-associated protein-2 in cultured cortical neurons.	2004	14698748
The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) project: an open-label pragmatic randomised control trial comparing the efficacy of differing therapeutic agents for primary care detoxification from either street heroin or methadone [ISRCTN07752728].	2004 Apr 29	15117415
Role of central sympathoexcitation in enhanced hypercapnic chemosensitivity in patients with heart failure.	2004 Dec	15632879
Guanfacine treatment of clozapine-induced sialorrhea.	2004 Dec	15538136
[Tourette syndrome: an analysis of its comorbidity and specific treatment].	2004 Feb	15011166
Pharmacological management of attention-deficit hyperactivity disorder.	2004 Jun	15163276
Evidence-based pharmacotherapy for attention-deficit hyperactivity disorder.	2004 Mar	14733627
Loss of glutamatergic pyramidal neurons in frontal and temporal cortex resulting from attenuation of FGFR1 signaling is associated with spontaneous hyperactivity in mice.	2004 Mar 3	14999075
Subtypes of alpha1- and alpha2-adrenoceptors mediating noradrenergic modulation of spontaneous inhibitory postsynaptic currents in the hypothalamic paraventricular nucleus.	2004 May	15117338
Potential noradrenergic targets for cognitive enhancement in schizophrenia.	2004 May	15115947
Noradrenergic alpha-2 agonists have anxiolytic-like actions on stress-related behavior and mesoprefrontal dopamine biochemistry.	2004 Nov 19	15494168
Methylphenidate an effective treatment for ADHD?	2004 Oct	15628613
Alpha2 adrenergic agonists for the management of opioid withdrawal.	2004 Oct 18	15495025
Clonidine and guanfacine-induced antinociception in visceral pain: possible role of alpha 2/I2 binding sites.	2004 Oct 6	15464067
Guanfacine treatment of hyperactivity and inattention in pervasive developmental disorders: a retrospective analysis of 80 cases.	2004 Summer	15319020
Nonstimulant therapies for attention-deficit hyperactivity disorder (ADHD) in children and adults.	2005	16222911
Alpha-2 adrenoceptor activation inhibits phencyclidine-induced deficits of spatial working memory in rats.	2005 Aug	15714223
Impaired visuospatial divided attention in the spontaneously hypertensive rat.	2005 Feb 28	15639183
Locomotor hyperactivity induced by blockade of prefrontal cortical alpha2-adrenoceptors in monkeys.	2005 Jan 15	15652880
Aripiprazole in children and adolescents: clinical experience.	2005 Jul	16159529
G-protein-coupled alpha2A-adrenoreceptor agonists differentially alter citrus leaf and fruit abscission by affecting expression of ACC synthase and ACC oxidase.	2005 Jul	15928018
Yohimbine disrupts prepulse inhibition in rats via action at 5-HT1A receptors, not alpha2-adrenoceptors.	2005 Jul	15719216
Animal models of attention-deficit hyperactivity disorder.	2005 Jul 15	16022733
Neurobiology of executive functions: catecholamine influences on prefrontal cortical functions.	2005 Jun 1	15950011
The safety of non-stimulant agents for the treatment of attention-deficit hyperactivity disorder.	2005 Mar	15794722
An open-label, prospective study of guanfacine in children with ADHD and tic disorders.	2005 Nov	16856436
Recent pharmacologic updates.	2005 Oct	16262586
Central sympathetic inhibition augments sleep-related ultradian rhythm of parasympathetic tone in patients with chronic heart failure.	2005 Sep	16127185
Mechanism of action of agents used in attention-deficit/hyperactivity disorder.	2006	16961428
Introduction: new developments in the treatment of attention-deficit/hyperactivity disorder.	2006	16961423
Guanfacine produces differential effects in frontal cortex compared with striatum: assessed by phMRI BOLD contrast.	2006 Dec	17016709
New developments in the treatment of ADHD.	2006 Jan	16426101
Effect of noradrenergic system on the anxiolytic-like effect of DOI (5-HT2A/2C agonists) in the four-plate test.	2006 Jan	16307296
Noradrenergic modulation of space exploration in visual neglect.	2006 Jan	16261567
Yohimbine acts as a putative in vivo alpha2A/D-antagonist in the rat prefrontal cortex.	2006 Jul 24	16697527
Tourette's Syndrome.	2006 Jun	16650718
Syncope in children with Tourette's syndrome treated with guanfacine.	2006 Mar	16229000
Heme coordination states of unfolded ferrous cytochrome C.	2006 Oct 15	16877519
Relative contribution of intracellular and extracellular Ca2+ to alpha2-adrenoceptor-mediated contractions of ovine pulmonary artery.	2006 Sep	16787748
Differential noradrenergic influence on seizure expression in genetically Fast and Slow kindling rat strains during massed trial stimulation of the amygdala.	2007 Feb	17027042
The effects of guanfacine on context processing abnormalities in schizotypal personality disorder.	2007 May 15	16950221

Patents

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 Created by `admin` on `Fri Jun 25 21:59:17 UTC 2021` Edited by `admin` on `Fri Jun 25 21:59:17 UTC 2021`
Record UNII	30OMY4G3MK
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

GUANFACINE

Official Name

English

N-AMIDINO-2-(2,6-DICHLOROPHENYL)ACETAMIDE

Systematic Name

English

GUANFACINE [MI]

Common Name

English

GUANFACINE [VANDF]

Common Name

English

ESTULIC

Brand Name

English

GUANFACINE [INN]

Common Name

English

NSC-759121

Code

English

BENZENEACETAMIDE, N-(AMINOIMINOMETHYL)-2,6-DICHLORO-

Systematic Name

English

GUANFACINE [WHO-DD]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175554