Progesterone receptor antagonist is effective in relieving neuropathic pain.
Injury to the spinal nerves of mice induces allodynia and hyperalgesia. Intrathecal injection of the progesterone/estrogen receptor antagonist ICI 182,780 produced antinociceptive effects. Co-administration of estrogen did not reduce but tended to enhance the antinociceptive effect of ICI 182,780. On the other hand, co-administration of progesterone dose-dependently reduced the antinociceptive effect of ICI 182,780, indicating that the antinociceptive effect is through antiprogesterone receptor activity of ICI 182,780. These results suggest that spinal progesterone receptors play an important role in neuropathic pain, and that controlling the activity of progesterone receptors may be of great importance in the treatment of neuropathic pain.
Kondo
Daisuke
D
Department of Pharmacology and Neurobiology, Graduate School of Medicine, Tokyo Medical and Dental University, 1-5-45 Yushima, Bunkyo-ku, Tokyo 113-8519, Japan.
Yabe
Ritsuko
R
Kurihara
Takashi
T
Saegusa
Hironao
H
Zong
Shuqin
S
Tanabe
Tsutomu
T
D000700:Analgesics / Q000008:administration & dosage / Q000494:pharmacology; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004958:Estradiol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D004965:Estrogen Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D004967:Estrogens / Q000008:administration & dosage / Q000494:pharmacology; D000077267:Fulvestrant; D006358:Hot Temperature / Q000009:adverse effects; D006930:Hyperalgesia / Q000209:etiology / Q000503:physiopathology / Q000517:prevention & control; D007278:Injections, Spinal; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D009437:Neuralgia / Q000503:physiopathology / Q000517:prevention & control*; D010146:Pain / Q000209:etiology / Q000503:physiopathology / Q000517:prevention & control; D010147:Pain Measurement / Q000379:methods; D011374:Progesterone / Q000008:administration & dosage / Q000494:pharmacology; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors* / Q000502:physiology; D013127:Spinal Nerves / Q000293:injuries / Q000503:physiopathology
D000700:Analgesics; D004965:Estrogen Antagonists; D004967:Estrogens; D011980:Receptors, Progesterone; D000077267:Fulvestrant; D011374:Progesterone; D004958:Estradiol