guanfacine   Click here for help

GtoPdb Ligand ID: 522

Synonyms: Estulic® | Intuniv® | Tenex®
Approved drug
guanfacine is an approved drug (FDA (1986), EMA (2015))
Compound class: Synthetic organic
Comment: Guanfacine is a centrally acting sympatholytic drug acting via activation of α2-adrenoceptors.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 3
Topological polar surface area 81.47
Molecular weight 245.01
XLogP 2.04
No. Lipinski's rules broken 0
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Canonical SMILES O=C(Cc1c(Cl)cccc1Cl)N=C(N)N
Isomeric SMILES O=C(Cc1c(Cl)cccc1Cl)N=C(N)N
InChI 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)
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Summary of Clinical Use Click here for help
Guanfacine is used to treat hypertension, ADHD and anxiety.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Guanfacine is an α2-adrenoceptor agonist with some selectivity for the α2A-AR. Guanfacine-induced central α-adrenergic stimulation evokes reduced sympathetic outflow to the heart, kidneys, and peripheral vasculature and results in reduced systolic and diastolic blood pressure, and reduced heart beat rate. Guanfacine is also used as a non-psychostimulant treatment for ADHD, either alone or in combination with psychostimulant therapy. Although ADHD medications work through different mechanisms, the common underlying effect of modulating catecholamine transmission in the pre-frontal cortex (PFC) is believed to be responsible for the relief of ADHD symptoms (eg deficits in planning, organization, working memory, and response inhibition).
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