Dual action calcium-sensing receptor modulator unmasks novel mode-switching mechanism

KJ Gregory, I Kufareva, AN Keller… - ACS pharmacology & …, 2018 - ACS Publications
… NPS2143 weakly inhibited Ca 2+ o potency (2-fold) (Figure 3d … of the ligand core dictates
PAM versus NAM activity. For … poses due to its flexible trans-1,2-disubstituted cyclohexane ring…

[HTML][HTML] Signalling pathways involved in the detection of peptones by murine small intestinal enteroendocrine L-cells

R Pais, FM Gribble, F Reimann - Peptides, 2016 - Elsevier
… the calcium sensing receptor CaSR in peptone sensing in … In the presence of Calhex 231
hydrochloride (10 μM) which … In this study, we observed a strong inhibition of the peptone-…

Targeting human astrocytes' calcium-sensing receptors for treatment of Alzheimer's disease

A Chiarini, U Armato, JF Whitfield… - Current Pharmaceutical …, 2017 - ingentaconnect.com
N1-Benzoyl-N2-[1-(1naphthyl)ethyl]-trans-1, 2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide
(Calhex 231) as a new calcium

Fluorescent sensors for imaging of interstitial calcium

AA Valiente-Gabioud… - Nature …, 2023 - nature.com
Calcium Sensing Receptor (CaSR), a G-protein coupled receptor that, among other ligands,
… The crystals were cryoprotected with addition of 30% of ethylene glycol and flash-frozen in …

[HTML][HTML] Family C G-protein-coupled receptors in Alzheimer's disease and therapeutic implications

I Dal Prà, U Armato, A Chiarini - Frontiers in pharmacology, 2019 - frontiersin.org
… Finally, neutral allosteric ligands (NALs) bind their sequence on a receptor but do not …
selective calcium-sensing receptor (CaSR) negative allosteric modulators (NAMs) (or calcilytics). …