An estrogen receptor-beta agonist is active in models of inflammatory and chemical-induced pain.
ERB-041 (2-(3-Fluoro-4-hydroxyphenyl)-7-vinyl-1,3 benzoxazol-5-ol) is a selective estrogen receptor-beta agonist with activity in rodent models of rheumatoid arthritis and endometriosis. Clinical trials for these diseases are underway: however, the role of estrogen receptor-beta in modulating pain associated with inflammation remains unknown. These studies demonstrate that acutely administered ERB-041 is anti-hyperalgesic in preclinical models of chemical-induced and acute inflammatory pain, thus suggesting that ERB-041 may be useful for modulating pain associated with some types of inflammation.
Leventhal
Liza
L
Neuroscience Discovery Research, Wyeth Research, Princeton, NJ 08543, United States.
Brandt
Michael R
MR
Cummons
Terri A
TA
Piesla
Michael J
MJ
Rogers
Kathryn E
KE
Harris
Heather A
HA
D000818:Animals; D004305:Dose-Response Relationship, Drug; D004958:Estradiol / Q000031:analogs & derivatives / Q000494:pharmacology; D047629:Estrogen Receptor beta / Q000819:agonists*; D000077267:Fulvestrant; D006358:Hot Temperature; D006930:Hyperalgesia / Q000188:drug therapy; D007249:Inflammation / Q000139:chemically induced* / Q000150:complications; D008297:Male; D010080:Oxazoles / Q000494:pharmacology*; D010146:Pain / Q000139:chemically induced* / Q000209:etiology; D051381:Rats; D017207:Rats, Sprague-Dawley
C478102:ERB 041; D047629:Estrogen Receptor beta; D010080:Oxazoles; D000077267:Fulvestrant; D004958:Estradiol