Investigation of sigma receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines

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Abstract

A series of polymethyl-substituted piperidines linked to either a 6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl or a 6-methoxynaphthalen-1-yl moiety was generated with the aim of verifying a previously generated hypothesis: tetralin and naphthalene nuclei confer opposite activity at the 1 receptor. Compounds 6, 9 and 10 displayed appreciable affinity at both  subtypes, but none of the novel compounds displayed significant antiproliferative activity in MCF7wt and MCF71 cell lines. The effect on bradikynin-triggered Ca2+ mobilization was studied as a methodology to suggest sigma receptors mediated activity.

Autore Pugliese

Tutti gli autori

  • ABATE C.;BERARDI F.;GASPARRE G.;CASSANO G.;NISO M.;PERRONE R.;FERORELLI S.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2013

ISSN

0968-0896

ISBN

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Numero di citazioni Wos

3

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

3

Ultimo Aggiornamento Citazioni

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Settori ERC

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Codici ASJC

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