219928-13-9Relevant articles and documents
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor
Bertini, Simone,Chicca, Andrea,Gado, Francesca,Arena, Chiara,Nieri, Daniela,Digiacomo, Maria,Saccomanni, Giuseppe,Zhao, Pingwei,Abood, Mary E.,Macchia, Marco,Gertsch, Jürg,Manera, Clementina
, p. 6427 - 6434 (2017)
In this work, we explored the molecular framework of the known CB1R allosteric modulator PSNCBAM-1 with the aim to generate new bioactive analogs and to deepen the structure-activity relationships of this type of compounds. In particular, the introduction
Silicon-based rhodamine fluorescent staining reagent as well as preparation method and application thereof
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Paragraph 0105-0110, (2021/01/29)
The invention discloses a silicon-based rhodamine fluorescent staining reagent as well as a preparation method and application thereof, and belongs to the field of organic chemistry and biochemistry.According to the silicon-based rhodamine fluorescent staining reagent as well as preparation method and application thereof of the invention, a silicon atom substituted rhodamine derivative is used asa basic frame, and is modified with aromatic amines in different forms, so that the silicon-based rhodamine fluorescent staining reagent which has large Stokes shift and high fluorescence intensity and can mark immunoglobulin IgG can be synthesized, so that the silicon-based rhodamine fluorescent staining reagent can be used for in-vitro SARS-CoV2-virus specific antibody fluorescence ELISA detection. The silicon-based rhodamine fluorescence staining reagent has large Stokes shift (greater than 140 nm), can effectively avoid mutual interference of excitation light and emitted light, and is high in detection sensitivity; a fluorescence ELISA detection method established based on the fluorescence antibody can be suitable for microplate readers with different bandwidths, and is wide in application range.
PSNCBAM-1 analogs: Structural evolutions and allosteric properties at cannabinoid CB1 receptor
Meini, Serena,Gado, Francesca,Stevenson, Lesley A.,Digiacomo, Maria,Saba, Alessandro,Codini, Simone,Macchia, Marco,Pertwee, Roger G.,Bertini, Simone,Manera, Clementina
, (2020/07/20)
Allosteric modulation of the CB1Rs could represent an alternative strategy for the treatment of diseases in which these receptors are involved, without the undesirable effects associated with their orthosteric stimulation. PSNCBAM-1 is a reference diaryl urea derivative that positively affects the binding affinity of orthosteric ligands (PAM) and negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs. In this work we reported the design, synthesis and biological evaluation of three different series of compounds, derived from structural modifications of PSNCBAM-1 and its analogs reported in the recent literature. Almost all the new compounds increased the percentage of binding affinity of CP55940 at CB1Rs, showing a PAM profile. When tested alone in the [35S]GTPγS functional assay, only a few derivatives lacked detectable activity, so were tested in the same functional assay in the presence of CP55940. Among these, compounds 11 and 18 proved to be functional NAMs at CB1Rs, dampening the orthosteric agonist-induced receptor functionality by approximately 30percent. The structural features presented in this work provide new CB1R-allosteric modulators (with a profile similar to the reference compound PSNCBAM-1) and an extension of the structure-activity relationships for this type of molecule at CB1Rs.