Poor interaction of some quinolizidine derivatives with dopamine D1- and D2- type receptors.
The displacement of [3H]SCH-23390 and of [3H]spiperone from striatal, dopamine D1- and D2-type receptors by several quinolizidinyl-derivatives of bi- and tricyclic systems was investigated. All tested compounds did not affect SCH-23390 binding and exhibited only weak activity on spiperone binding to D2 binding sites (Ki = 1.9 microM). Therefore the good deconditioning activity (CAR blockade in rats) of 6-chloro-1-lupinyl-3-methyl-quinoxalinone (18) must rely on interactions with other kinds of receptors.
Sparatore
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A
Istituto Chimico Farmaceutico e Tossicologico, Università di Milano.
Vaccari
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A
Boido
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V
Spartore
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F
D000818:Animals; D001552:Benzazepines / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D066298:In Vitro Techniques; D017072:Neostriatum / Q000187:drug effects / Q000378:metabolism; D011807:Quinolizines / Q000494:pharmacology*; D051381:Rats; D017447:Receptors, Dopamine D1 / Q000187:drug effects*; D017448:Receptors, Dopamine D2 / Q000187:drug effects*; D013134:Spiperone / Q000494:pharmacology
D001552:Benzazepines; D011807:Quinolizines; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D013134:Spiperone