title: Investigation of σ receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.
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 σ1 receptor. Compounds 6, 9 and 10 displayed appreciable affinity at both σ subtypes, but none of the novel compounds displayed significant antiproliferative activity in MCF7wt and MCF7σ1 cell lines. The effect on bradikynin-triggered Ca(2+) mobilization was studied as a methodology to suggest σ receptors mediated activity.
authors: Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari ALDO MORO, Via Orabona 4, I-70125 Bari, Italy.
authors: Mauro
authors: M
authors: Niso
authors: Carmen
authors: C
authors: Abate
authors: Savina
authors: S
authors: Ferorelli
authors: Giuseppe
authors: G
authors: Cassano
authors: Giuseppe
authors: G
authors: Gasparre
authors: Roberto
authors: R
authors: Perrone
authors: Francesco
authors: F
authors: Berardi
mesh_terms: D002118:Calcium / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D006801:Humans; D008745:Methylation; D009281:Naphthalenes / Q000737:chemistry* / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*; D017480:Receptors, sigma / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000494:pharmacology
chemical_list: D009281:Naphthalenes; D010880:Piperidines; D017480:Receptors, sigma; D013764:Tetrahydronaphthalenes; D002118:Calcium