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Poor interaction of some quinolizidine derivatives with dopamine D1- and D2- type receptors.

Anna Sparatore, Andrea Vaccari, Vito Boido, F. Spartore

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Abstract

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.

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What this paper is about

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.

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Available abstract

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.

Key concepts: Spiperone, Chemistry, SCH-23390, Dopamine receptor, Dopamine receptor D2, Receptor, Tricyclic, Stereochemistry

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Poor interaction of some quinolizidine derivatives with dopamine D1- and D2- type receptors. — Research Paper | ScholarLens