Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics.
A series of 3-aminoethyl-1-tetralones, conformationally constrained higher homologues of haloperidol (standard for typical antipsychotic profile), have been obtained by a four-step route from valerolactone. Their binding affinities at dopamine D(2) and serotonin 5-HT2A and 5-HT2C receptors were determined, showing in some cases an atypical antipsychotic profile.
Alvarado
Mario
M
Departamento de Química Orgánica, Laboratorio de Química Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela. E-15782, Santiago de Compostela, Spain.
Coelho
Alberto
A
Masaguer
Christian F
CF
Raviña
Enrique
E
Brea
José
J
Padín
J Fernando
JF
Loza
María I
MI
D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000378:metabolism*; D001665:Binding Sites; D006220:Haloperidol / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000378:metabolism*; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D044348:Receptors, Serotonin, 5-HT2 / Q000378:metabolism; D044024:Tetralones / Q000138:chemical synthesis* / Q000378:metabolism*
D014150:Antipsychotic Agents; D017448:Receptors, Dopamine D2; D044348:Receptors, Serotonin, 5-HT2; D044024:Tetralones; D006220:Haloperidol