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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.

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publishing date
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
2020-07-29 06:02:26
@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},
}