Guanfacine HCl

  • Chemical Properties
CAS No. 29110-48-3 Cat. No. BCP21710
Name Guanfacine HCl
Synonyms BS 100-141; BS-100-141; BS100-141; SPD-503; SPD 503; SPD503; Guanfacine hydrochloride;
Formula C9H10Cl3N3O M. Wt 282.55
  • Biological Activity
Description Guanfacine Hcl, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.Guanfacine, also known as BS 100-141 and SPD-503, is a sympatholytic drug used in the treatment of attention deficit hyperactivity disorder (ADHD) and hypertension (not to be confused with guaifenesin, an expectorant). It is a selective α2A receptor agonist. These receptors are concentrated heavily in the prefrontal cortex and the locus coeruleus, with the potential to improve attention resulting from interaction with receptors in the former. Guanfacine lowers both systolic and diastolic blood pressure by activating the central nervous system α2A norepinephrine autoreceptors, which results in reduced peripheral sympathetic outflow and thus a reduction in peripheral sympathetic tone. Guanfacine is currently approved and marketed in the United States[8] and Europe[9] as Intuniv for the treatment of ADHD in children and adolescents aged 6–18 years.
Pathways Neuro Signaling Pathway GPCR/G Protein 
Targets Adrenergic Receptor 

Structure

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