A calcimimetic and positive allosteric modulator of CaSR
CaSR biased allosteric modulator (pEC50 = 7.8-8.1). Calcimimetic. Displays ability to bias signalling towards the accumulation of pERK1/2 and IP1. Reduces parathyroid hormone (PTH) levels in rat serum without inducing the release of calcitonin. Exhibits no significant activation of human GABAB or type I PTH receptors. Orally active.
Cook et al (2015) Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics. Br.J.Pharmacol. 172 185 PMID:25220431 |Ma et al (2011) Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor. J.Pharmacol.Exp.Ther. 337 275 PMID:21239511 |Leach et al (2016) Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor. Cell.Res. 26 574 PMID:27002221
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