• Title/Summary/Keyword: 486

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THE USE OF MIFEPRISTONE (RU486) IN THE TREATMENT OF PSYCHOTIC MAJOR DEPRESSION

  • Her, Song
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2007.04a
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    • pp.25-44
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    • 2007

  • The glucocorticoid receptor (GR) is an intracellular protein that is widely distributed throughout hippocampal and neocortical brain tissue. Mifepristone (RU486) is a potent GR antagonist that has also been shown to exhibit partial agonist-like effects. The precise location of the GR domain involved in the agonist-like activity of RU486 is unknown. Here, we examine this aspect of GR signaling by comparing human GR (hGR) construct with a Guyanese squirrel monkey GR (gsmGR) construct in which nuclear translocation and transactivation are known to be impaired. Using an objective translocation scoring method, we found that both hGR and gsmGR are translocated by RU486, and that nuclear translocation of hGR is significantly increased compared to gsmGR at 10 nM, 100 nM and 1000 nM RU486 in transiently transfected COS1 cells. While addition of RU486 to the cells transfected with hGR results in a 16-fold dose-dependent increase in transactivation compared to non-treated cells, no significant change in transactivation is observed with gsmGR at doses up to 100 nM RU486. Further experiments using six GR chimeras indicate that replacement of the hGR carboxyl-terminus of tau-1 transactivation domain (C-AF1, amino acids 132-428) with that from gsmGR diminishes hGR transactivation by RU486. These results demonstrate that RU486-induced transactivation of GR is determined in part by amino acids in the C-AF1 domain.

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Effects of Antiprogesterone (RU486) and Antiestrogen (Tamoxifen) on Ovulatory Response and Oocyte Quality in Rats Primed with Pregnant Mare Serum Gonadotropin (PMSG 전처리한 쥐에 있어서 Antiprogesterone(RU486)과 Antiestrogen(Tamoxifen)이 배란과 Oocyte에 미치는 영향)

  • 윤영원;권종국;유규연
    • Journal of Embryo Transfer
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    • v.4 no.1
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    • pp.46-55
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    • 1989

  • The effects of an antiprogesterone (RU 486) and an antiestrogen (tamoxifen) on ovulatory response and oocyte morphology were examined in pregnant mare serum gonadotropin (PMSG)-primed immatare female rats (28 days of age): a comparison has been made on two different regirnens primed with a "control" dose (4 IU) and a "superovulatory" dose (40 IU) of PMSG. Females for control control regimen received three consecutive injections of lmg RU486, lmg tamoxifen, or vehicle at 24, 36 and 48hr, and were killed at 72l'r after PMSG. Animals for superovalatory regimen received lmg RU486, 2.5mg tamoxifen, or vehicle fouowlag the injection schedule comparable to control regimen, and were killed at 60 and 72hr after PMSG. Compared to vehicle group, there was a significant reduction in ovulatory response as judged by the proportion of rats ovulating andi or by the mean number of oocytes per rat for each treatment of RU486 and tamoxifen in both regimens. The activity of tamoxifen in inhibiting the ovulatory response was greater in control, but less in superovulatory regimen than that of RU486 based on the dose employed for each antisteroid. In both regimens, RU 486 did not have any effect 6n the changes in the proportion of degenerate oocytes as well as ovarian weight, well tamoxifen treatment resulted in a marked promotion of oocyte degeneration as well as a great reduction in ovarian weight, compared to each parameter of vehicle group. RU486 treatment in each regimen did not alter the serum levels of any steroid hormones observed. Howerver, tamoxifen treatment was associated with significant increases in serum 17$\beta$-estradiol and decreases in progesterone in both regimens; also significant increases in androgens in superovulatory regimen. The results illustrate the relative inhibitory activity of RU486 and tamoxifen indicating major steroid hormone involved in PMSG-induced ovulation: 17$\beta$-estradiol for control and progesterone for superovulatory regimen. It also appears that tamoxifen-associated elevation of circulating 17$\beta$-estradiol andi or androgens could be in part, a contributing factor to the promotion of oocyte degeneration presumably by producing a hostile oviductal environment after ovulation.ent after ovulation.

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RU486 Suppresses Progesterone-induced Acrosome Reaction in Boar Spermatozoa

  • Jang, Sun-Phil;YiLee, S.H.
    • BMB Reports
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    • v.35 no.6
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    • pp.604-608
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    • 2002

  • The effects of progesterone on the acrosome reaction, as well as the effects of RU486 on the progesterone-induced acrosome reaction in capacitated boar spermatozoa, were investigated. Progesterone, a major steroid that is secreted by the cumulus cells of oocyte, clearly induced the acrosome reaction in a dose-dependent manner in capacitated boar spermatozoa, even though it failed to show similar effects in non-capacitated spermatozoa. RU486, a potent antiprogestin, significantly reduced the effects of progesterone on the progesterone-induced acrosome reaction; however, when treated alone, it showed no inhibitory effects on the acrosome reaction. The inhibitory effects of RU486 were also shown to be dose-dependent. These results imply that in addition to the well-known inducer of the acrosome reaction, zona pellucida, progesterone can also induce the acrosome reaction through its specific receptors on spermatozoa after the spermatozoa undergo capacitation.

  • https://doi.org/10.5483/BMBRep.2002.35.6.604 인용 PDF

의지의 치과인

  • The Korean Dental Association
    • The Journal of the Korean dental association
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    • v.17 no.7 s.122
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    • pp.486-486
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    • 1979

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