Discovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols
Gustafsson, Magnus LU ; Jensen, Jacob LU ; Bertozzi, Sine M. ; Currier, Erika A. ; Ma, Jian Nong ; Burstein, Ethan S. and Olsson, Roger LU
(2010)
In Bioorganic and Medicinal Chemistry Letters
20(19).
p.5918-5921
- 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.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/85eb3705-cbdc-40f5-9e00-5abc571e577b
- author
- Gustafsson, Magnus
LU
; Jensen, Jacob
LU
; Bertozzi, Sine M.
; Currier, Erika A.
; Ma, Jian Nong
; Burstein, Ethan S.
and Olsson, Roger
LU
- publishing date
- 2010-10-01
- type
- Contribution to journal
- publication status
- published
- 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
- in
- Bioorganic and Medicinal Chemistry Letters
- volume
- 20
- issue
- 19
- pages
- 4 pages
- publisher
- Elsevier
- external identifiers
-
- pmid:20727747
- scopus:77957578720
- ISSN
- 0960-894X
- DOI
- 10.1016/j.bmcl.2010.07.077
- language
- English
- LU publication?
- no
- id
- 85eb3705-cbdc-40f5-9e00-5abc571e577b
- date added to LUP
- 2019-10-02 09:35:34
- date last changed
- 2024-04-16 21:14:46
@article{85eb3705-cbdc-40f5-9e00-5abc571e577b,
abstract = {{<p>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.</p>}},
author = {{Gustafsson, Magnus and Jensen, Jacob and Bertozzi, Sine M. and Currier, Erika A. and Ma, Jian Nong and Burstein, Ethan S. and Olsson, Roger}},
issn = {{0960-894X}},
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}},
language = {{eng}},
month = {{10}},
number = {{19}},
pages = {{5918--5921}},
publisher = {{Elsevier}},
series = {{Bioorganic and Medicinal Chemistry Letters}},
title = {{Discovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols}},
url = {{http://dx.doi.org/10.1016/j.bmcl.2010.07.077}},
doi = {{10.1016/j.bmcl.2010.07.077}},
volume = {{20}},
year = {{2010}},
}