Structure-affinity relationship studies on arylpiperazine derivatives related to quizapine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor (Articolo in rivista)

Type

• Prodotto della ricerca (Classe)
• Articolo in rivista (Classe)

Label

• Structure-affinity relationship studies on arylpiperazine derivatives related to quizapine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor (Articolo in rivista) (literal)

Anno

• 2005-01-01T00:00:00+01:00 (literal)

Alternative label

• Cappelli A. 1, Giuliani G. 1, Gallelli A. 1, Valenti S. 1, Anzini M. 1, Mennuni L. 2, Makovec F. 2, Cupello A. 3, Vomero S. 1 (2005)
  Structure-affinity relationship studies on arylpiperazine derivatives related to quizapine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor
  in Bioorganic & medicinal chemistry (Print)
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Cappelli A. 1, Giuliani G. 1, Gallelli A. 1, Valenti S. 1, Anzini M. 1, Mennuni L. 2, Makovec F. 2, Cupello A. 3, Vomero S. 1 (literal)

Pagina inizio

• 3455 (literal)

Pagina fine

• 3460 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 13 (literal)

Rivista

• Bioorganic & medicinal chemistry (Rivista)

Note

• ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• 1. Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita` di Siena, Siena, Italy 2. Rotta Research Laboratorium S.p.A., Monza (MI), Italy 3. Istituto di Bioimmagini e Fisiologia Molecolare, CNR, Sezione di Genova, Genova, Italy (literal)

Titolo

• Structure-affinity relationship studies on arylpiperazine derivatives related to quizapine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor (literal)

Abstract

• A series of quipazine derivatives, previously synthesized to probe the 5-HT(3) receptor, was evaluated for its potential interaction with serotonin transporter (SERT). Some of them show nanomolar affinity for the rodent SERT comparable to or slightly higher than quipazine or N-methylquipazine. Subsequently a candidate was selected on the basis of its SERT affinity and submitted to a molecular manipulation of the basic moiety. The structure-affinity relationships obtained provided information on the role of the fused benzene ring of quipazine in the interaction with the SERT binding site and on the stereoelectronic requirements for the interaction of both the heteroaromatic component and the basic moiety. Moreover, the comparison of the structure-affinity relationships obtained in the present work with those concerning the interaction of these heteroarylpiperazine derivatives with 5-HT3 receptor suggested some molecular determinants of the selectivity SERT/5HT3 receptor. (literal)

Prodotto di

• Institute of molecular bioimaging and physiology (IBFM) (Istituto)
• Neurofisiopatologia e clinica (ME.P02.003.001) (Modulo)

Autore CNR

• AROLDO CUPELLO (Unità di personale interno)

Insieme di parole chiave

• Keywords of "Structure-affinity relationship studies on arylpiperazine derivatives related to quizapine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor" (Insieme di parole chiave)

Incoming links:

Prodotto

• Institute of molecular bioimaging and physiology (IBFM) (Istituto)
• Neurofisiopatologia e clinica (ME.P02.003.001) (Modulo)

Autore CNR di

• AROLDO CUPELLO (Unità di personale interno)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• Bioorganic & medicinal chemistry (Rivista)

Insieme di parole chiave di

• Keywords of "Structure-affinity relationship studies on arylpiperazine derivatives related to quizapine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor" (Insieme di parole chiave)