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G1043

Sigma-Aldrich

Guanfacine hydrochloride

≥98% (HPLC)

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Synonym(s):
N (Aminoiminomethyl)-2,6-dichlorobenzeneacetamide
Empirical Formula (Hill Notation):
C9H9Cl2N3O · HCl
CAS Number:
29110-48-3
Molecular Weight:
282.55
MDL number:
MFCD00798230
UNSPSC Code:
12352200
PubChem Substance ID:
24278452
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

color

white

solubility

H2O: soluble 12 mg/mL at 60 °C

originator

Promius

SMILES string

Cl.NC(=N)NC(=O)Cc1c(Cl)cccc1Cl

InChI

1S/C9H9Cl2N3O.ClH/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13;/h1-3H,4H2,(H4,12,13,14,15);1H

InChI key

DGFYECXYGUIODH-UHFFFAOYSA-N

Gene Information

human ... ADRA2A(150) , ADRA2B(151) , ADRA2C(152)

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Application

Guanfacine hydrochloride has been used as an α2A adrenoceptor agonist to test its protective effect on hypobaric hypoxia (HH) and in rat brain to measure blood oxygenation level dependent (BOLD) response.

Biochem/physiol Actions

Guanfacine stimulates the brain postsynaptic α2 adrenergic receptor (AR) and mediates the prefrontal cortical (PFC) neuronal regulation and strengthens their network. Guanfacine improves the density of neuronal dendrites and is useful in treating neuropsychiatric disorders. It modulates the synaptic and cytoskeletal proteins expression in prefrontal cortical (PFC) neurons and may improve hypobaric hypoxia (HH) induced PFC dysfunctions. Guanfacine enhances cognitive function and is recommended for attention deficit hyperactivity disorder (ADHD) therapy.
α-2 noradrenergic receptor agonist.

Features and Benefits

This compound was developed by Promius. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Sophie Duong et al.
Expert opinion on drug metabolism & toxicology, 8(5), 543-552 (2012-03-15)
Pharmacotherapy is frequently used to treat symptoms of attention-deficit/hyperactivity disorder (ADHD), the most common neurobehavioral disorder of childhood. The typically prescribed agents for ADHD have varying durations of effect and degrees of efficacy. The broad range of pharmacological treatments available
Guanfacine produces differential effects in frontal cortex compared with striatum: assessed by phMRI BOLD contrast
Easton N, et al.
Psychopharmacology, 189(3), 369-385 (2006)
Sandra Bond Chapman et al.
The journals of gerontology. Series A, Biological sciences and medical sciences, 67(7), 773-780 (2012-05-10)
Human cognitive aging has been too long neglected and underappreciated for its critical importance to quality of life in old age. The articles in this session present novel approaches to improving cognitive function in normal aging persons with drugs and
Yuanyuan Li et al.
Bioanalysis, 3(22), 2501-2514 (2011-11-30)
Dried blood spot (DBS) technology was evaluated for the quantitative determination of guanfacine in human blood in clinical studies. A very sensitive DBS assay has been developed using HPLC coupled with an AB Sciex 5500 QTRAP® (Applied Biosystems/MDS Sciex, ON
Kurt P Schulz et al.
Psychopharmacology, 226(2), 261-271 (2012-10-23)
Functional interactions between limbic regions that process emotions and frontal networks that guide response functions provide a substrate for emotional cues to influence behavior. Stimulation of postsynaptic α₂ adrenoceptors enhances the function of prefrontal regions in these networks. However, the
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