Discovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols

Research output: Contribution to journalArticle

Abstract

1-(Benzothiazol-2-yl)-1-(4-chlorophenyl)ethanol (1) was identified as a positive allosteric modulator (PAM) of the CaSR in a functional cell-based assay. This compound belongs to a class of compounds that is structurally distinct from other known positive allosteric modulators, for example, the phenylalkylamines cinacalcet, a modified analog (13) potently suppressed parathyroid hormone (PTH) release in rats, consistent with its profile as a PAM of CaSRs.

Details

Authors
  • Magnus Gustafsson
  • Jacob Jensen
  • Sine M. Bertozzi
  • Erika A. Currier
  • Jian Nong Ma
  • Ethan S. Burstein
  • Roger Olsson
External organisations
  • ACADIA Pharmaceuticals AB
  • ACADIA Pharmaceuticals Inc.
Research areas and keywords

Keywords

  • 1-(benzothiazol-2-yl)-1-phenylethanols, Allosteric, Calciumsensing receptor, Calindol, CaSR, Cinacalcet, Fendiline, GPCR, Hyperparathyroidism, In vivo, Modulators, PAM, Parathyroid hormone, SAR, Structure-activity relationship
Original languageEnglish
Pages (from-to)5918-5921
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number19
Publication statusPublished - 2010 Oct 1
Publication categoryResearch
Peer-reviewedYes
Externally publishedYes