Novel calcium sensing receptor ligands: a patent survey
L Kiefer, S Leiris, RH Dodd - Expert Opinion on Therapeutic Patents, 2011 - Taylor & Francis
… 7) in which one of the phenyl rings is replaced by a 1-naphthyl … potent new calcilytics. Starting
from the general formula 56, … the development of calhex 231, one of the first calcilytics to be …
from the general formula 56, … the development of calhex 231, one of the first calcilytics to be …
Allosteric modulation of the calcium-sensing receptor
AA Jensen, H Brauner-Osborne - Current neuropharmacology, 2007 - ingentaconnect.com
… Calhex 231 (N1-(4-Chlorobenzoyl)-N2-[1-(1-naphtyl)ethyl]trans-1,2-diaminocyclohexane),
one of the most potent … in the binding of the calcilytics NPS 2143 and Calhex 231 and the …
one of the most potent … in the binding of the calcilytics NPS 2143 and Calhex 231 and the …
Development of a calcium-sensing receptor molecular imaging agent
AM Yusof, S Kothandaraman, X Zhang, M Saji… - Surgery, 2013 - Elsevier
… of a known calcilytic compound, Calhex-231. Human … ring opening (B) with (R)-1-(1-naphthyl)
ethylamine (C) was a simple … From Fig 1 we have successfully synthesized Calhex 231 …
ethylamine (C) was a simple … From Fig 1 we have successfully synthesized Calhex 231 …
Molecular determinants of non-competitive antagonist binding to the mouse GPRC6A receptor
H Faure, T Gorojankina, N Rice, P Dauban, RH Dodd… - Cell calcium, 2009 - Elsevier
… Here we report that the calcimimetic Calindol and the calcilytic … :Calindol(R)-2-[1-(1-naphthyl)
ethylaminomethyl]-1H-indole. (… We have shown previously that Calhex 231 and NPS 2143 …
ethylaminomethyl]-1H-indole. (… We have shown previously that Calhex 231 and NPS 2143 …
Calcium-sensing receptor (CaSR): pharmacological properties and signaling pathways
AD Conigrave, DT Ward - Best practice & research Clinical endocrinology & …, 2013 - Elsevier
… the diversity of the receptor's ligands, ligand binding sites and … as well as the calcilytics NPS
2143 and Calhex 231.88, 103 … been demonstrated that signaling from pluripotent receptors …
2143 and Calhex 231.88, 103 … been demonstrated that signaling from pluripotent receptors …
Discovery and structure− activity relationships of trisubstituted pyrimidines/pyridines as novel calcium-sensing receptor antagonists
W Yang, Z Ruan, Y Wang, K Van Kirk… - Journal of medicinal …, 2009 - ACS Publications
… orally bioavailable small molecule calcilytic compound that … in potency from hydrogen (6b)
to methyl (6c) to ethyl (1). Some … 18d also demonstrated a desired in vivo activity profile by …
to methyl (6c) to ethyl (1). Some … 18d also demonstrated a desired in vivo activity profile by …
Agonists and allosteric modulators of the calcium-sensing receptor and their therapeutic applications
… tend to have higher potency. An orthosteric antagonist of the … ligands of the CaR, recent
studies have demonstrated that … On the other hand, calcilytics, such as NPS 2143 and Calhex 231…
studies have demonstrated that … On the other hand, calcilytics, such as NPS 2143 and Calhex 231…
Localization of CaSR antagonists in CaSR-expressing medullary thyroid cancer
H Ding, AM Yusof, S Kothandaraman… - The Journal of …, 2013 - academic.oup.com
… express high levels of calcium-sensing receptor (CaSR). The … We hypothesize that a
radiolabeled ligand to CaSR may … investigated the calcilytic potency of Calhex 231 and newly …
radiolabeled ligand to CaSR may … investigated the calcilytic potency of Calhex 231 and newly …
[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-…
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…
(Calhex 231) as a new calcium…