Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity.

Boy, Kenneth M; Dee, Michael; Yevich, Joseph; Torrente, John; Gao, Qi; Iben, Lawrence; Stark, Arlene; Mattson, Ronald J

Boy, Kenneth M; Dee, Michael; Yevich, Joseph; Torrente, John; Gao, Qi; Iben, Lawrence; Stark, Arlene; Mattson, Ronald J.

Afiliación

Boy KM; Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. boyk@bms.com

Bioorg Med Chem Lett ; 14(17): 4467-70, 2004 Sep 06.

Article en En | MEDLINE | ID: mdl-15357973

RESUMEN

Conformationally constrained aryl cyclohexanes and cyclohexenes based on aryl cyclohexanols 1 were prepared. Locking the aryl ring in plane with the cyclohexane moiety provided potent SSRIs 3. Conversely, fixing the aryl ring perpendicular to the cyclohexane ring via a spiro lactone provided balanced 5-HT1A antagonists with mid-nanomolar range SSRI potency (compounds 2).

Asunto(s)

Receptor de Serotonina 5-HT1A/metabolismo; Inhibidores Selectivos de la Recaptación de Serotonina/química; Inhibidores Selectivos de la Recaptación de Serotonina/metabolismo; Serotonina/metabolismo; Ligandos; Conformación Molecular

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Bases de datos: MEDLINE Asunto principal: Serotonina / Inhibidores Selectivos de la Recaptación de Serotonina / Receptor de Serotonina 5-HT1A Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2004 Tipo del documento: Article País de afiliación: Estados Unidos

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