α-Adrenergic receptor function, arousal and sleep: mechanisms and therapeutic implications.

Noradrenergic (NE) neurotransmission and particularly α-adrenergic receptor function has been identified as a critical component of the sleep/wake regulation in animals and humans. This work (i) provides an update on the impact of NE neurotransmission on the sleep/wake regulation, (ii) summarizes the effects of α-receptor agonists and antagonists on arousal and sleep in animals and healthy humans, and (iii) reviews the current body of evidence for the effectiveness and safety of these compounds in the treatment of clinical conditions characterized by alterations of arousal or sleep, including attention deficit and hyperactivity disorder (ADHD), post-traumatic stress disorder (PTSD), borderline personality disorder and primary sleep disorders. This systematic evaluation of the potential and limitations of the effects of α-adrenergic compounds might promote novel inroads for the treatment of these highly prevalent clinical conditions.