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Broad modulation of neuropathic pain states by a selective estrogen receptor beta agonist

Piu, Fabrice ; Cheevers, Cindy ; Hyldtoft, Lene ; Gardell, Luis R. ; Del Tredici, Andria L. ; Andersen, Carsten B. ; Fairbairn, Luke C. ; Lund, Birgitte W. ; Gustafsson, Magnus LU and Schiffer, Hans H. , et al. (2008) In European Journal of Pharmacology 590(1-3). p.423-429
Abstract

The effects of estrogens on pain perception remain controversial. In animal models, both beneficial and detrimental effects of non-selective estrogens have been reported. ERb-131 a non-steroidal estrogen receptor beta ligand was evaluated in several pain animal models involving nerve injury or sensitization. Using functional and binding assays, ERb-131 was characterized as a potent and selective estrogen receptor beta agonist. In vivo, ERb-131 was devoid of estrogen receptor alpha activity as assessed in a rat uterotrophic assay. ERb-131 alleviated tactile hyperalgesia induced by capsaicin, and reversed tactile allodynia caused by spinal nerve ligation and various chemical insults. Moreover, ERb-131 did not influence the pain threshold... (More)

The effects of estrogens on pain perception remain controversial. In animal models, both beneficial and detrimental effects of non-selective estrogens have been reported. ERb-131 a non-steroidal estrogen receptor beta ligand was evaluated in several pain animal models involving nerve injury or sensitization. Using functional and binding assays, ERb-131 was characterized as a potent and selective estrogen receptor beta agonist. In vivo, ERb-131 was devoid of estrogen receptor alpha activity as assessed in a rat uterotrophic assay. ERb-131 alleviated tactile hyperalgesia induced by capsaicin, and reversed tactile allodynia caused by spinal nerve ligation and various chemical insults. Moreover, ERb-131 did not influence the pain threshold of normal healthy animals. Thus, estrogen receptor beta agonism is a critical effector in attenuating a broad range of anti-nociceptive states.

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publishing date
type
Contribution to journal
publication status
published
keywords
Agonist, Estrogen receptor beta, Neuropathic pain
in
European Journal of Pharmacology
volume
590
issue
1-3
pages
423 - 429
publisher
Elsevier
external identifiers
  • scopus:48049099210
  • pmid:18559275
ISSN
0014-2999
DOI
10.1016/j.ejphar.2008.05.015
language
English
LU publication?
no
id
2e4cc103-3b23-4f97-86a1-7a83d6f1f1d6
date added to LUP
2019-10-02 10:22:52
date last changed
2020-11-29 05:12:04
@article{2e4cc103-3b23-4f97-86a1-7a83d6f1f1d6,
  abstract     = {<p>The effects of estrogens on pain perception remain controversial. In animal models, both beneficial and detrimental effects of non-selective estrogens have been reported. ERb-131 a non-steroidal estrogen receptor beta ligand was evaluated in several pain animal models involving nerve injury or sensitization. Using functional and binding assays, ERb-131 was characterized as a potent and selective estrogen receptor beta agonist. In vivo, ERb-131 was devoid of estrogen receptor alpha activity as assessed in a rat uterotrophic assay. ERb-131 alleviated tactile hyperalgesia induced by capsaicin, and reversed tactile allodynia caused by spinal nerve ligation and various chemical insults. Moreover, ERb-131 did not influence the pain threshold of normal healthy animals. Thus, estrogen receptor beta agonism is a critical effector in attenuating a broad range of anti-nociceptive states.</p>},
  author       = {Piu, Fabrice and Cheevers, Cindy and Hyldtoft, Lene and Gardell, Luis R. and Del Tredici, Andria L. and Andersen, Carsten B. and Fairbairn, Luke C. and Lund, Birgitte W. and Gustafsson, Magnus and Schiffer, Hans H. and Donello, John E. and Olsson, Roger and Gil, Daniel W. and Brann, Mark R.},
  issn         = {0014-2999},
  language     = {eng},
  month        = {08},
  number       = {1-3},
  pages        = {423--429},
  publisher    = {Elsevier},
  series       = {European Journal of Pharmacology},
  title        = {Broad modulation of neuropathic pain states by a selective estrogen receptor beta agonist},
  url          = {http://dx.doi.org/10.1016/j.ejphar.2008.05.015},
  doi          = {10.1016/j.ejphar.2008.05.015},
  volume       = {590},
  year         = {2008},
}