920463-20-3Relevant academic research and scientific papers
New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation
Zampieri, Daniele,Romano, Maurizio,Menegazzi, Renzo,Mamolo, Maria Grazia
, p. 3206 - 3209 (2018)
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.
[35S]GTPγS binding studies of amphiphilic drugs-activated Gi proteins: A caveat
Manetti, Dina,Mannelli, Lorenzo Di Cesare,Dei, Silvia,Guandalini, Luca,Martini, Elisabetta,Banchelli, Martina,Ghelardini, Carla
supporting information; experimental part, p. 2224 - 2229 (2009/12/07)
This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [35S]GTPγS to different subtypes of Gi protein. The problem arose from the strong affinity between [35S]GTPγS and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results.
