title: Substituted 3-amino and/or 3-aminomethyl-3,4-dihydro-2H-1-benzopyrans: synthesis and biological activity.
abstract: A series of new 3-amino, 3-aminomethyl-5-alkoxy-3,4-dihydro-2H-1-benzopyran and 5'-alkoxy-3',4'-dihydrospiro-[piperazine-2.3'(2'H)-benzopyran] derivatives was prepared and evaluated for affinity at 5-HT1A, 5-HT2A and D2 receptors. Two of the compounds (1f and 2b) can be considered as potent and selective 5-HT2A ligands. One compound (1g) demonstrated high affinity for 5-HT1A and D2 receptor binding sites and one compound (1d) proved to be a mixed 5-HT1A/5-HT2A ligand.
authors.affiliation: Institut de Chimie Organique et Analytique, associé all CNRS, Université d'Orleans, France.
authors.forename: C
authors.initials: C
authors.lastname: Comoy
authors.forename: V
authors.initials: V
authors.lastname: Guérin
authors.forename: B
authors.initials: B
authors.lastname: Pfeiffer
authors.forename: M C
authors.initials: MC
authors.lastname: Rettori
authors.forename: P
authors.initials: P
authors.lastname: Renard
authors.forename: G
authors.initials: G
authors.lastname: Guillaumet
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D001665:Binding Sites; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D001578:Benzopyrans; D008024:Ligands; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; C088154:3,4-dihydro-3-amino-2H-1-benzopyran