| HOME | HELP | CONTACT US | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
|
|
|
|||||||
|
|||||||||
ZM 189,154 ([1RS,2RS]-2-(4-hydroxyphenyl)-2-methyl -1-[9-(4,4,5,5,5-penta-fluoropentyl)sulphinylnonyl]-1,2, 3,4-tetrahydronaphth-6-ol) is a non-steroidal pure anti-oestrogen. It has a high relative affinity for the oestrogen receptor, completely blocks the trophic action of oestradiol (OE2) on the uterus in immature and ovariectomized (OVX) adult rats and, in the latter, also completely blocks the trophic action of OE2 on vagina, bone and growth rate. ZM 189,154 displays no intrinsic oestrogen-agonist activity on uterus, vagina, bone, LH secretion or growth rate in OVX rats. Differential sensitivity of OE2-regulated processes was more apparent in intact rats. Daily doses of 0·6 mg/kg per day of ZM 189,154 blocked ovulation; 2 mg/kg per day achieved maximal uterine atrophy but did not affect bone density or growth rate; 10 mg/kg per day produced a broader spectrum of effects (reduced bone density, increased basal LH, slightly increased growth rate), but the magnitude of these was smaller than after ovariectomy; the 10 mg/kg dose also produced multiple ovarian follicular cysts. The failure of ZM 189,154 to achieve complete ovariectomy-like effects in intact rats may be due to the action of ovarian factors other than OE2, or to the circulating OE2 levels resulting from the disturbance to ovarian function posing too strong a challenge to the antagonist.
Journal of Endocrinology (1994) 141, 335–341
This article has been cited by other articles:
|
|
 |
|
  S. F. Palter, A. B. Tavares, A. Hourvitz, J. D. Veldhuis, and E. Y. Adashi Are Estrogens of Import to Primate/Human Ovarian Folliculogenesis? Endocr. Rev., June 1, 2001; 22(3): 389 - 424. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. F. Couse, D. O. Bunch, J. Lindzey, D. W. Schomberg, and K. S. Korach Prevention of the Polycystic Ovarian Phenotype and Characterization of Ovulatory Capacity in the Estrogen Receptor-{alpha} Knockout Mouse Endocrinology, December 1, 1999; 140(12): 5855 - 5865. [Abstract] [Full Text]
|
|
|
|
 |
|
 I Slater, J Odum, and J Ashby Resveratrol and red wine consumption Human and Experimental Toxicology, October 1, 1999; 18(10): 625 - 626. [PDF]
|
|
|
|
|
|
J. F. Couse and K. S. Korach Estrogen Receptor Null Mice: What Have We Learned and Where Will They Lead Us? Endocr. Rev., June 1, 1999; 20(3): 358 - 417. [Abstract] [Full Text]
|
|
|
|
|
|
D. W. Schomberg, J. F. Couse, A. Mukherjee, D. B. Lubahn, M. Sar, K. E. Mayo, and K. S. Korach Targeted Disruption of the Estrogen Receptor-{alpha} Gene in Female Mice: Characterization of Ovarian Responses and Phenotype in the Adult Endocrinology, June 1, 1999; 140(6): 2733 - 2744. [Abstract] [Full Text]
|
|
|
|
 |
|
 C. S. Rosenfeld, X. Yuan, M. Manikkam, M. D. Calder, H. A. Garverick, and D. B. Lubahn Cloning, Sequencing, and Localization of Bovine Estrogen Receptor-ß within the Ovarian Follicle Biol Reprod, March 1, 1999; 60(3): 691 - 697. [Abstract] [Full Text]
|
|
|
|
 |
|
 J. I. Macgregor and V. C. Jordan Basic Guide to the Mechanisms of Antiestrogen Action Pharmacol. Rev., June 1, 1998; 50(2): 151 - 196. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Sourla, S. Luo, C. Labrie, A. Belanger, and F. Labrie Morphological Changes Induced by 6-Month Treatment of Intact and Ovariectomized Mice with Tamoxifen and the Pure Antiestrogen EM-800 Endocrinology, December 1, 1997; 138(12): 5605 - 5617. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. A. Jimenez, D. E. Magee, H. U. Bryant, and R. T. Turner Clomiphene Prevents Cancellous Bone Loss from Tibia of Ovariectomized Rats Endocrinology, May 1, 1997; 138(5): 1794 - 1800. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. Korach Insights from the study of animals lacking functional estrogen receptor Science, December 2, 1994; 266(5190): 1524 - 1527. [Abstract] [PDF]
|
|
| HOME | HELP | CONTACT US | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
