Discovery of selective nonpeptidergic neuropeptide FF2 receptor agonists
Gaubert, Gilles ; Bertozzi, Fabio ; Kelly, Nicholas M. ; Pawlas, Jan ; Scully, Audra L. ; Nash, Norman R. ; Gardell, Luis R. ; Lameh, Jelveh and Olsson, Roger LU
(2009)
In Journal of Medicinal Chemistry
52(21).
p.6511-6514
- Abstract
We report the discovery and initial characterization of a novel class of selective NPFF2 agonists. HTS screening using R-SAT, a whole cell based functional assay, identified a class of aryliminoguanidines as NPFF1 and NPFF2 ligands. Subsequent optimization led to molecules exhibiting selective NPFF2 agonistic activity. Systemic administration showed that selective NPFF2 agonists (1 and 3) are active in various pain models in vivo, whereas administration of a nonselective NPFF1 and NPFF2 agonist (9) increases sensitivity to noxious and non-noxious stimuli.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/94294210-2787-4cf3-ba71-e6a3b0bc294c
- author
- Gaubert, Gilles
; Bertozzi, Fabio
; Kelly, Nicholas M.
; Pawlas, Jan
; Scully, Audra L.
; Nash, Norman R.
; Gardell, Luis R.
; Lameh, Jelveh
and Olsson, Roger
LU
- publishing date
- 2009-11-12
- type
- Contribution to journal
- publication status
- published
- in
- Journal of Medicinal Chemistry
- volume
- 52
- issue
- 21
- pages
- 6511 - 6514
- publisher
- The American Chemical Society (ACS)
- external identifiers
-
- pmid:19803524
- scopus:71049144430
- ISSN
- 0022-2623
- DOI
- 10.1021/jm9011998
- language
- English
- LU publication?
- no
- id
- 94294210-2787-4cf3-ba71-e6a3b0bc294c
- date added to LUP
- 2019-10-02 09:43:27
- date last changed
- 2024-10-02 14:08:50
@article{94294210-2787-4cf3-ba71-e6a3b0bc294c,
abstract = {{<p>We report the discovery and initial characterization of a novel class of selective NPFF2 agonists. HTS screening using R-SAT, a whole cell based functional assay, identified a class of aryliminoguanidines as NPFF1 and NPFF2 ligands. Subsequent optimization led to molecules exhibiting selective NPFF2 agonistic activity. Systemic administration showed that selective NPFF2 agonists (1 and 3) are active in various pain models in vivo, whereas administration of a nonselective NPFF1 and NPFF2 agonist (9) increases sensitivity to noxious and non-noxious stimuli.</p>}},
author = {{Gaubert, Gilles and Bertozzi, Fabio and Kelly, Nicholas M. and Pawlas, Jan and Scully, Audra L. and Nash, Norman R. and Gardell, Luis R. and Lameh, Jelveh and Olsson, Roger}},
issn = {{0022-2623}},
language = {{eng}},
month = {{11}},
number = {{21}},
pages = {{6511--6514}},
publisher = {{The American Chemical Society (ACS)}},
series = {{Journal of Medicinal Chemistry}},
title = {{Discovery of selective nonpeptidergic neuropeptide FF2 receptor agonists}},
url = {{http://dx.doi.org/10.1021/jm9011998}},
doi = {{10.1021/jm9011998}},
volume = {{52}},
year = {{2009}},
}