Effect of the new potent LHRH antagonist antide

Habenicht, U.‐F.; Schneider, M. R.; Etreby, M. F. El

doi:10.1016/0960-0760(90)90447-s

Cited by 24 publications

(5 citation statements)

References 12 publications

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“…Atrophic changes in the prostate and testis have been reported in male rats treated with antide (Habenicht et al 1990b), but the histological changes in the female sex organs have not yet been studied. The morphometric examination revealed a smaller follicle size in the ovary of rats given antide than in the control, and granulosa cell fragmentation and follicular atresia had increased.…”

Section: Discussionmentioning

confidence: 97%

Immature uterotrophic assay of estrogenic compounds in rats given diets of different phytoestrogen content and the ovarian changes with ICI 182,780 or antide

Yamasaki

Sawaki

Noda

et al. 2002

Archives of Toxicology

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To investigate the influence of phyotestrogens in the diet, an immature uterotrophic assay of ethinylestradiol, bisphenol A, 4-nonylphenol or genistein was performed in rats given the formula MF diet, modified NIH-07 open formula diet, or modified NIH-07 phytoestrogen-lowered-diet (study 1). The chemicals were administered subcutaneously from 20 days of age for 3 days. Doses of ethinylestradiol, bisphenol A, 4-nonylphenol or genistein were 0.06-0.6 micro g/kg per day, 1-10 mg/kg per day, 10-100 mg/kg per day or 1-20 mg/kg per day, respectively. In another study, an immature uterotrophic assay of genistein and ethinylestradiol together with ICI 182,780 or antide was performed to compare the ovarian changes with these chemicals (study 2). Doses of genistein or ethinylestradiol were 30 mg/kg per day or 0.6 micro g/kg per day, respectively, and these chemicals were injected subcutaneously from 20 days of age for 3 days. In study 1, there were no essential differences in the uterus weights among the various phytoestrogen-content diets. In study 2, the ovary weights in rats given genistein were significantly higher than in the controls, whereas the ovary weights in rats given ethinylestradiol were lower than in the controls. The ovary weights in the ICI 182,780 plus genistein group were significantly higher than in the genistein group, but decrease of the ovary weights was detected in the antide plus genistein group. There was no significant difference in ovary weights between the ICI 182,780 plus ethinylestradiol group and the ethinylestradiol group, but decrease of ovary weights was detected in antide plus ethinylestradiol group. In a histological examination of the ovary, fluid-filled follicles in the genistein group were more numerous than in other groups and increase of granulosa cell fragmentation was seen in the ethinylestradiol and other groups with the exception of the genistein group. The present findings demonstrate that the sensitivity of the immature rat uterotrophic assay is not influenced by the relatively low level of phytoestrogen in diets and that the ovarian changes occurring with genistein and ethinylestradiol are different.

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Section: Discussionmentioning

confidence: 97%

Immature uterotrophic assay of estrogenic compounds in rats given diets of different phytoestrogen content and the ovarian changes with ICI 182,780 or antide

Yamasaki

Sawaki

Noda

et al. 2002

Archives of Toxicology

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“…Antide was chosen as a potent specific GnRH‐I receptor antagonist based on its ability to block GnRH‐I induced gonadotropin secretion in the rat and monkey (42). In the current study, antide did not activate an inositol phosphate response in COS‐7 cells transfected with the marmoset GnRH‐II receptor, indicating that it possesses minimal agonistic activity, unlike some other related GnRH analogues (29).…”

Section: Discussionmentioning

confidence: 99%

Evidence That Gonadotropin‐Releasing Hormone II Is Not a Physiological Regulator of Gonadotropin Secretion in Mammals

Gault

Maudsley

Lincoln

2003

J Neuroendocrinology

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Gonadotropin-releasing hormone (GnRH)-II stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion when administered at high doses in mammals, and this effect has been assumed to be mediated through the GnRH-II receptor expressed on gonadotropes. This study used two selective GnRH-I receptor antagonists to test the alternative hypothesis that GnRH-II acts through the GnRH-I receptor to elicit gonadotropin secretion. The antagonist, antide, was used to characterize the receptor-relay because it was a pure antagonist in vitro based on inositol phosphate responses in COS-7 cells transfected with either mammalian GnRH-I and GnRH-II receptors and, in vivo, potently antagonized the gonadotropin-releasing effect of a single injection of 250 ng GnRH-I in our sexually inactive sheep model. In a series of studies in sheep, antide (i). blocked the acute LH response to a single injection of GnRH-II (20 microg antide: 10 microg GnRH-II); (ii). blocked both the acute, pulsatile LH response and the FSH priming response to 2-hourly injections of GnRH-II over 36 h (100 microg antide/8 h: 4 microg GnRH-II/2 h); and (iii). chronically blocked both the pulsatile LH response and the marked FSH priming response to 4-hourly injections of GnRH-II over 10 days (75 microg antide/8 h: 4 microg GnRH-II/4 h). In two final experiments, the GnRH-I antagonist 135-18, shown previously to agonize the mammalian GnRH-II receptor, blocked the gonadotropin-releasing effects of GnRH-I (250 ng) but failed to elicit an LH response when given alone, and simultaneous administration of GnRH-II (250 ng) failed to alter the LH-releasing effect of GnRH-I (50-500 ng). These data thus support our hypothesis. Based on additional literature, it is unlikely that the GnRH-II decapeptide is a native regulator of the gonadotrope in mammals.

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“…Three sets of subjects were produced: (i) females (n = 14) that were treated on PND 28 and 42 with a gonadotrophin‐releasing hormone (GnRH) peptide antagonist, Antide (Bachem, Germany), via s.c. injection at a dose of 6 mg kg ‐1 in 1:1 propylene glycol: saline solution, as in our previous research 61 (injection volumes [μL] were 2× animal weight [g]); (ii) females (n = 14) that received vehicle (propylene glycol: saline solution) injections on PND 28 and 42; and (iii) males (n = 14) that received vehicle injections on PND 28 and 42 (as a result of practical constraints, four males received the first injection on PND 29 rather than PND 28). Each bolus of Antide was predicted to suppress circulating gonadal hormone levels for between 2 and 3 weeks, as in previous studies, 61,62 and so the regime of two injections 14 days apart was designed to suppress gonadal hormone levels from the late juvenile phase through to the end of late adolescence (age ranges based on previous studies 18,63 ). No more than five animals from each litter were assigned to a single experimental group, and, in the majority of cases, no more than four females from a single litter were used as subjects in the experiment (ie, two Antide‐treated females and two control females), with all subjects paired with a littermate in the same experimental group.…”

Section: Methodsmentioning

confidence: 99%

Suppression of ovarian hormones in adolescent rats has no effect on anxiety‐like behaviour or c‐fos activation in the amygdala

Hodgson

Richmond

Tello

et al. 2020

J Neuroendocrinology

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Effect of the new potent LHRH antagonist antide

Cited by 24 publications

References 12 publications

Immature uterotrophic assay of estrogenic compounds in rats given diets of different phytoestrogen content and the ovarian changes with ICI 182,780 or antide

Immature uterotrophic assay of estrogenic compounds in rats given diets of different phytoestrogen content and the ovarian changes with ICI 182,780 or antide

Evidence That Gonadotropin‐Releasing Hormone II Is Not a Physiological Regulator of Gonadotropin Secretion in Mammals

Suppression of ovarian hormones in adolescent rats has no effect on anxiety‐like behaviour or c‐fos activation in the amygdala

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