Ligand id: 522

Name: guanfacine

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 3
Topological polar surface area 81.47
Molecular weight 245.01
XLogP 1.56
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Guanfacine is used to treat hypertension, ADHD and anxiety.
Mechanism Of Action and Pharmacodynamic Effects
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).