Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics |
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| Authors: | Alvarado Mario Coelho Alberto Masaguer Christian F Raviña Enrique Brea José Padín J Fernando Loza María I |
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| Affiliation: | Departamento de Química Orgánica, Laboratorio de Química Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela. E-15782, Santiago de Compostela, Spain. |
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| Abstract: | 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. |
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