Discovery of the first nonpeptide agonist of the GPR14/Urotensin-II receptor : 3-(4-Chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one (AC-7954)
Croston, Glenn E. ; Olsson, Roger LU
; Currier, Erika A.
; Burstein, Ethan S.
; Weiner, David
; Nash, Norman
; Severance, Daniel
; Allenmark, Stig G.
; Thunberg, Linda
and Ma, Jian Nong
, et al.
(2002)
In Journal of Medicinal Chemistry
45(23).
p.4950-4953
- Abstract
A functional cell-based screen identified 3-(4-chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one hydrochloride (AC-7954, 1) as a nonpeptidic agonist of the urotensin-II receptor. Racemic 1 had an EC50 of 300 nM at the human UII receptor and was highly selective. Testing of the enantiopure (+)- and (-)-1 revealed that the UII receptor activity of racemic 1 resides primarily in (+)-1. Being a selective nonpeptidic druglike UII receptor agonist, (+)-1 will be useful as a pharmacological research tool and a potential drug lead.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/919c0ec4-4c1f-479e-b5b8-725b60802da2
- author
- Croston, Glenn E.
; Olsson, Roger
LU
; Currier, Erika A.
; Burstein, Ethan S.
; Weiner, David
; Nash, Norman
; Severance, Daniel
; Allenmark, Stig G.
; Thunberg, Linda
and Ma, Jian Nong
, et al. (More)
- Croston, Glenn E.
; Olsson, Roger
LU
; Currier, Erika A.
; Burstein, Ethan S.
; Weiner, David
; Nash, Norman
; Severance, Daniel
; Allenmark, Stig G.
; Thunberg, Linda
; Ma, Jian Nong
; Mohell, Nina
; O'Dowd, Brian
; Brann, Mark R.
and Hacksell, Uli
(Less)
- publishing date
- 2002-10-09
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Journal of Medicinal Chemistry
- volume
- 45
- issue
- 23
- pages
- 4950 - 4953
- publisher
- The American Chemical Society (ACS)
- external identifiers
-
- scopus:0037038316
- pmid:12408704
- ISSN
- 0022-2623
- DOI
- 10.1021/jm025551
- language
- English
- LU publication?
- no
- id
- 919c0ec4-4c1f-479e-b5b8-725b60802da2
- date added to LUP
- 2019-10-02 10:41:45
- date last changed
- 2024-01-08 13:59:45
@article{919c0ec4-4c1f-479e-b5b8-725b60802da2,
abstract = {{<p>A functional cell-based screen identified 3-(4-chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one hydrochloride (AC-7954, 1) as a nonpeptidic agonist of the urotensin-II receptor. Racemic 1 had an EC50 of 300 nM at the human UII receptor and was highly selective. Testing of the enantiopure (+)- and (-)-1 revealed that the UII receptor activity of racemic 1 resides primarily in (+)-1. Being a selective nonpeptidic druglike UII receptor agonist, (+)-1 will be useful as a pharmacological research tool and a potential drug lead.</p>}},
author = {{Croston, Glenn E. and Olsson, Roger and Currier, Erika A. and Burstein, Ethan S. and Weiner, David and Nash, Norman and Severance, Daniel and Allenmark, Stig G. and Thunberg, Linda and Ma, Jian Nong and Mohell, Nina and O'Dowd, Brian and Brann, Mark R. and Hacksell, Uli}},
issn = {{0022-2623}},
language = {{eng}},
month = {{10}},
number = {{23}},
pages = {{4950--4953}},
publisher = {{The American Chemical Society (ACS)}},
series = {{Journal of Medicinal Chemistry}},
title = {{Discovery of the first nonpeptide agonist of the GPR14/Urotensin-II receptor : 3-(4-Chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one (AC-7954)}},
url = {{http://dx.doi.org/10.1021/jm025551}},
doi = {{10.1021/jm025551}},
volume = {{45}},
year = {{2002}},
}