The sigma receptor (σR) family has been considered mysterious for a long time. In fact, the σ2R subtype has been cloned only recently, revealing its identity as TMEM97, a NPC1-binding protein involved in cholesterol biosynthesis and implicated in the pathogenesis of cancer and neurologic disorders. With the aim of developing new chemical entities gifted with σR affinity, herein we report the design and synthesis of new piperidine-based alkylacetamide derivatives with mixed affinity towards both σ1 and σ2R subtypes.

New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation

Zampieri, Daniele
;
Romano, Maurizio;Menegazzi, Renzo;Mamolo, Maria Grazia
2018-01-01

Abstract

The sigma receptor (σR) family has been considered mysterious for a long time. In fact, the σ2R subtype has been cloned only recently, revealing its identity as TMEM97, a NPC1-binding protein involved in cholesterol biosynthesis and implicated in the pathogenesis of cancer and neurologic disorders. With the aim of developing new chemical entities gifted with σR affinity, herein we report the design and synthesis of new piperidine-based alkylacetamide derivatives with mixed affinity towards both σ1 and σ2R subtypes.
2018
Pubblicato
https://www.sciencedirect.com/science/article/pii/S0960894X18306802
File in questo prodotto:
File Dimensione Formato  
1-s2.0-S0960894X18306802-main.pdf

Accesso chiuso

Tipologia: Documento in Versione Editoriale
Licenza: Copyright Editore
Dimensione 285.64 kB
Formato Adobe PDF
285.64 kB Adobe PDF   Visualizza/Apri   Richiedi una copia
1-s2.0-S0960894X18306802-mmc1.pdf

Accesso chiuso

Descrizione: supplementary material
Tipologia: Altro materiale allegato
Licenza: Copyright Editore
Dimensione 702.22 kB
Formato Adobe PDF
702.22 kB Adobe PDF   Visualizza/Apri   Richiedi una copia
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11368/2928953
Citazioni
  • ???jsp.display-item.citation.pmc??? 0
  • Scopus 2
  • ???jsp.display-item.citation.isi??? 2
social impact