Broad modulation of neuropathic pain states by a selective estrogen receptor beta agonist
(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.
(Less)
- author
- publishing date
- 2008-08-20
- 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
-
- pmid:18559275
- scopus:48049099210
- 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
- 2024-01-01 21:27:53
@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}}, keywords = {{Agonist; Estrogen receptor beta; Neuropathic pain}}, 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}}, }