Intact 5HT neuroterminals are not required for 5HT2 receptor down-regulation by amitriptyline.
Chronic treatment of rats with the antidepressant, amitriptyline, resulted in a reduced number of cerebral cortical 5HT2 receptors measured as cinanserin displaceable [3H] spiperone binding. Pretreatment of rats with the serotonergic neurotoxin, p-chloroamphetamine, did not inhibit the effects of subsequent chronic amitriptyline treatment on 5HT2 receptor density whilst still severe neuroterminal destruction. It is suggested that such data indicate a post-synaptic locus of action for amitriptyline and have implications in regard to current concepts of antidepressant action.
D000639:Amitriptyline / Q000494:pharmacology*; D000818:Animals; D007700:Kinetics; D008297:Male; D009411:Nerve Endings / Q000378:metabolism*; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects*; D012701:Serotonin / Q000502:physiology*; D013134:Spiperone / Q000494:pharmacology
D011985:Receptors, Serotonin; D000639:Amitriptyline; D012701:Serotonin; D013134:Spiperone