Deep transcranial magnetic stimulation in major depression: Safety and feasibility open study Conference Paper uri icon


  • Objective: Alpha2 adrenoceptors mediate the negative feedback noradrenaline elicits on its own transmission. Furthermore, alpha2 adrenoceptors are found on corticolimbic serotonergic, dopaminergic and cholinergic projections. Blockade of alpha2 adrenoceptors should lead to enhanced neurotransmission in all these systems. Combining serotonin (5- HT) reuptake inhibition with alpha2-adrenoceptor blockade is therefore expected to be more effective than 5-HT reuptake inhibition alone. Results: R226161 is a potent in vitro and in vivo 5-HT uptake inhibitor and alpha2-adrenoceptor antagonist. It binds preferentially to the human alpha2C adrenoceptor subtype (Ki= 0.27 nM) and is 6-and 11-times less potent in binding to the human alpha2B and 2A adrenoceptors. Furthermore, R226161 binds to the h5-HT transporter with Ki= 1.25 nM. The compound has good central penetration and ex …

publication date

  • July 1, 2008