The use of α-2A adrenergic agonists for the treatment of attention-deficit/hyperactivity disorder

Expert Rev Neurother. 2010 Oct;10(10):1595-605. doi: 10.1586/ern.10.133.

Abstract

Neuropsychiatric disorders involve dysfunction of the prefrontal cortex (PFC), a highly evolved brain region that mediates executive functioning. The dorsolateral PFC is specialized for regulating attention and behavior, while the ventromedial PFC is specialized for regulating emotion. These abilities arise from PFC pyramidal cell networks that excite each other to maintain goals and rules 'in mind'. Imaging studies have shown reduced PFC gray matter, weaker PFC connections and altered PFC function in patients with attention-deficit/hyperactivity disorder. Thus, medications that strengthen PFC network connections may be particularly useful for the treatment of attention-deficit/hyperactivity disorder and related disorders. Recent data show that compounds such as guanfacine can enhance PFC function by stimulating postsynaptic α-2A receptors on the dendritic spines of PFC pyramidal cells where networks interconnect. Stimulation of these receptors inhibits cAMP signaling, thus closing potassium channels and strengthening physiological connections. These actions may benefit patients with weak PFC function.

Publication types

  • Review

MeSH terms

  • Adrenergic alpha-2 Receptor Agonists / therapeutic use*
  • Attention / drug effects
  • Attention / physiology
  • Attention Deficit Disorder with Hyperactivity / drug therapy*
  • Attention Deficit Disorder with Hyperactivity / genetics
  • Attention Deficit Disorder with Hyperactivity / physiopathology*
  • Behavior / drug effects
  • Behavior / physiology
  • Catecholamines / metabolism
  • Catecholamines / physiology
  • Emotions / drug effects
  • Emotions / physiology
  • Humans
  • Prefrontal Cortex / metabolism
  • Prefrontal Cortex / physiology
  • Prefrontal Cortex / physiopathology
  • Receptors, Adrenergic, alpha-2 / metabolism*
  • Receptors, Adrenergic, alpha-2 / physiology

Substances

  • Adrenergic alpha-2 Receptor Agonists
  • Catecholamines
  • Receptors, Adrenergic, alpha-2