Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds.

摘要: The synthesis of 5-(dipropylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij] quinolin-2(1H)-one (5), a potent dopamine D2 agonist showing high dopamine/serotonin (5HT1A) selectivity, is described. Dopaminergic activity associated with the (R)-enantiomer 5; (S)-enantiomer shows no dopaminergic activity. A series analogues where imidazolone ring was modified to various 5- or 6-membered heterocyclic rings were prepared. Some these compounds showed combination and serotonergic activity, while one compound, 6-(dipropylamino)-1,2,6,7-tetrahydro-3H,5H-pyrido[3,2,1- ij]quinazolin-3-one (24), selective agonist. Various 5 dipropylamine substituent Most reduced several as at serotonin 5HT1A receptor. Orientations for new receptors are proposed compared those other tricyclic ligands known have affinity receptors.