The acute effect of sertindole on brain 5-HT2, D2 and alpha 1 receptors (ex vivo radioreceptor binding studies).
The ability of sertindole to influence the ex vivo binding of 3H-ketanserin, 3H-prazosin and 3H-spiperone to 5-HT2 receptors, alpha 1-adrenoceptors and DA D2 receptors, respectively, in rat brain has been studied after acute treatment. Sertindole is a potent, long acting compound which readily passes the blood-brain barrier. It dose-dependently binds to all three receptors types. In line with in vivo behavioural experiments sertindole has the most pronounced effect on 5-HT2 receptors, lower effect on alpha 1-adrenoceptors and the lowest effect on striatal D2 receptors.
Hyttel
J
J
H. Lundbeck A/S, Copenhagen, Denmark.
Nielsen
J B
JB
Nowak
G
G
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D007093:Imidazoles / Q000494:pharmacology*; D007211:Indoles / Q000494:pharmacology*; D007650:Ketanserin / Q000378:metabolism; D008297:Male; D011224:Prazosin / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects* / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000187:drug effects* / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism
D007093:Imidazoles; D007211:Indoles; D011942:Receptors, Adrenergic, alpha; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D012701:Serotonin; D013134:Spiperone; D007650:Ketanserin; C066304:sertindole; D011224:Prazosin