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Search results for: Rabbit anti Androgen Receptor (pSer213)

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#33995571   2019/03/24 To Up

Eplerenone as a treatment for resistant hypertension in pregnancy.

Mineralocorticoid receptor antagonists are highly effective in the management of resistant hypertension and primary hyperaldosteronism. Recent studies demonstrate that mineralocorticoid receptor antagonists significantly reduce blood pressure, severity of obstructive sleep apnoea and arterial stiffness in patients with resistant hypertension and moderate-severe obstructive sleep apnoea. Eplerenone is a selective mineralocorticoid receptor antagonist that does not act as an androgen receptor blocker, thus reducing the risk of fetal anti-androgenic effects. Rat and rabbit studies demonstrated that when exposed to 30 times the equivalent therapeutic human dose, 100 mg/day, there were no teratogenic or demasculinisation effects. To date, the use of eplerenone has been reported in six human pregnancies in women with Gitelman syndrome, primary hyperaldosteronism and cardiac failure, in which no teratogenic effects were seen. Described here is a case of resistant hypertension associated with obstructive sleep apnoea in pregnancy, treated with eplerenone. The potential role of using eplerenone in pregnancy as treatment for resistant hypertension is discussed. Not applicable.
Jessica Gehlert, Adam Morton

2226 related Products with: Eplerenone as a treatment for resistant hypertension in pregnancy.

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#33461196   2021/01/18 To Up

Tissue Expression of Androgen Receptor Splice Variant 7 at Radical Prostatectomy Predicts Risk of Progression in Untreated Nonmetastatic Prostate Cancer.

Androgen receptor splice variant V7 (AR-V7) was recently detected in circulating tumor cells of castration-resistant prostate cancer (PC) patients and its expression correlated with resistance to new-generation androgen signaling inhibitors.
Alessandro Sciarra, Martina Maggi, Stefano Salciccia, Alice Nicolai, Elisabetta Tortorella, Sabrina Giantulli, Fabio Massimo Magliocca, Ida Silvestri, Ludovica Taglieri, Susanna Cattarino, Susanna Scarpa

2645 related Products with: Tissue Expression of Androgen Receptor Splice Variant 7 at Radical Prostatectomy Predicts Risk of Progression in Untreated Nonmetastatic Prostate Cancer.



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#31769454   // To Up

A novel cell membrane-cloaked magnetic nanogripper with enhanced stability for drug discovery.

Cell membrane-cloaked nanotechnology has attracted increasing attention owing to its unique bionic properties, such as specific recognition and biocompatibility conferred by the integrated membrane structure and receptors. However, this technology is limited by the dissociation of the cell membrane from its carrier. Here, we report a novel type of cell membrane-cloaked modified magnetic nanoparticle with good stability in drug discovery. High α1A-adrenergic receptor (α1A-AR) expressing HEK293 cell membrane-cloaked magnetic nanogrippers (α1A/MNGs) were used as a platform for the specific targeting and binding of α1A-AR antagonists as candidate bioactive compounds from traditional Chinese medicine (TCM). Furthermore, using a dynamic covalent bonding approach, α1A/MNGs showed great stability with positive control drug recoveries of α1A/MNGs showing almost no decline after use in five adsorption-desorption cycles. Moreover, the α1A/MNGs possessed a unilamellar membrane with magnetic features and exhibited good binding capacity and selectivity. Ultimately, TCM and pharmacological studies of the bioactivity of the screened compounds confirmed the considerable targeting and binding capability of α1A/MNGs. Application of aldehyde group modification in this drug-targeting concept further improved biomaterial stability and paves the way for the development of new drug discovery strategies. More importantly, the successful application of α1A/MNGs provides new insights into methodologies to improve the integration of cell membranes with the nanoparticle platform.
Yusi Bu, Qi Hu, Xiaolin Zhang, Ting Li, Xiaoyu Xie, Sicen Wang

2121 related Products with: A novel cell membrane-cloaked magnetic nanogripper with enhanced stability for drug discovery.

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#28316975   2017/02/21 To Up

Role of Estrogens in the Size of Neuronal Somata of Paravaginal Ganglia in Ovariectomized Rabbits.

We aimed to determine the role of estrogens in modulating the size of neuronal somata of paravaginal ganglia. Rabbits were allocated into control (C), ovariectomized (OVX), and OVX treated with estradiol benzoate (OVX + EB) groups to evaluate the neuronal soma area; total serum estradiol (E2) and testosterone (T) levels; the percentage of immunoreactive (ir) neurons anti-aromatase, anti-estrogen receptor (ER, ER) and anti-androgen receptor (AR); the intensity of the immunostaining anti-glial cell line-derived neurotrophic factor (GDNF) and the GDNF family receptor alpha type 1 (GFR1); and the number of satellite glial cells (SGCs) per neuron. There was a decrease in the neuronal soma size for the OVX group, which was associated with low T, high percentages of aromatase-ir and neuritic AR-ir neurons, and a strong immunostaining anti-GDNF and anti-GFR1. The decrease in the neuronal soma size was prevented by the EB treatment that increased the E2 without affecting the T levels. Moreover, there was a high percentage of neuritic AR-ir neurons, a strong GDNF immunostaining in the SGC, and an increase in the SGCs per neuron. Present findings show that estrogens modulate the soma size of neurons of the paravaginal ganglia, likely involving the participation of the SGC.
Laura G Hernández-Aragón, Verónica García-Villamar, María de Los Ángeles Carrasco-Ruiz, Leticia Nicolás-Toledo, Arturo Ortega, Estela Cuevas-Romero, Margarita Martínez-Gómez, Francisco Castelán

2651 related Products with: Role of Estrogens in the Size of Neuronal Somata of Paravaginal Ganglia in Ovariectomized Rabbits.

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#27611647   2016/09/09 To Up

Immunohistochemical Localization of Luteinizing Hormone Receptor in the Cyclic Gilt Ovary.

Luteinizing hormone receptor (LHR) is a specific membrane receptor on the granulosa and theca cells that bind to luteinizing hormone (LH), resulting in androgen and progesterone production. Hence, the regulation of LHR expression is necessary for follicle maturation, ovulation and corpus luteum formation. We examined the immunolocalization of LHR in cyclic gilt ovaries. The ovaries were obtained from 21 gilts aged 326.0 ± 38.7 days and weighing 154.6 ± 15.7 kg. The ovarian tissues were incubated with rabbit anti-LHR polyclonal antibody. The follicles were categorized as primordial, primary, preantral and antral follicles. Ovarian phase was categorized as either follicular or luteal phases. The immunolocalization of LHR was clearly expressed in primary, preantral and antral follicles. LHR immunostaining was detected in the cytoplasm of granulosa, theca interna and luteal cells. LHR immunostaining was evaluated using imaging software. LHR immunostaining in the theca interna cells in antral follicles was almost twice as intense as that in preantral follicles (65.4% versus 38.3%, P < 0.01). LHR immunostaining was higher in the follicular phase than in the luteal phase (58.6% versus 45.2%, P < 0.05). In conclusion, the expression of LHR in the theca interna cells of antral follicles in the follicular phase was higher than in the luteal phase. The expression of LHR in all types of the follicles indicates that LHR may impact follicular development from the primary follicle stage onwards.
D Phoophitphong, S Srisuwatanasagul, P Tummaruk

2139 related Products with: Immunohistochemical Localization of Luteinizing Hormone Receptor in the Cyclic Gilt Ovary.

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#26073023   2015/06/11 To Up

Pharmacological profile of CS-3150, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.

The present study was designed to characterize the pharmacological profile of CS-3150, a novel non-steroidal mineralocorticoid receptor antagonist. In the radioligand-binding assay, CS-3150 inhibited (3)H-aldosterone binding to mineralocorticoid receptor with an IC50 value of 9.4nM, and its potency was superior to that of spironolactone and eplerenone, whose IC50s were 36 and 713nM, respectively. CS-3150 also showed at least 1000-fold higher selectivity for mineralocorticoid receptor over other steroid hormone receptors, glucocorticoid receptor, androgen receptor and progesterone receptor. In the reporter gene assay, CS-3150 inhibited aldosterone-induced transcriptional activation of human mineralocorticoid receptor with an IC50 value of 3.7nM, and its potency was superior to that of spironolactone and eplerenone, whose IC50s were 66 and 970nM, respectively. CS-3150 had no agonistic effect on mineralocorticoid receptor and did not show any antagonistic or agonistic effect on glucocorticoid receptor, androgen receptor and progesterone receptor even at the high concentration of 5μM. In adrenalectomized rats, single oral administration of CS-3150 suppressed aldosterone-induced decrease in urinary Na(+)/K(+) ratio, an index of in vivo mineralocorticoid receptor activation, and this suppressive effect was more potent and longer-lasting than that of spironolactone and eplerenone. Chronic treatment with CS-3150 inhibited blood pressure elevation induced by deoxycorticosterone acetate (DOCA)/salt-loading to rats, and this antihypertensive effect was more potent than that of spironolactone and eplerenone. These findings indicate that CS-3150 is a selective and highly potent mineralocorticoid receptor antagonist with long-lasting oral activity. This agent could be useful for the treatment of hypertension, cardiovascular and renal disorders.
Kiyoshi Arai, Tsuyoshi Homma, Yuka Morikawa, Naoko Ubukata, Hiyoyuki Tsuruoka, Kazumasa Aoki, Hirokazu Ishikawa, Makoto Mizuno, Toshio Sada

1024 related Products with: Pharmacological profile of CS-3150, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.

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#25461902   2014/10/22 To Up

Structural features of endocrine active chemicals--A comparison of in vivo and in vitro data.

Studies on reproductive toxicity need high numbers of test animals. Therefore, we investigated whether chemical structural features (SF) in combination with in vitro data on specific adverse outcome pathways (AOPs) may be used for predicting reproductive toxicity of untested chemicals. Using the OECD Toolbox and expert judgment, we identified 89 structure groups for 275 chemicals for which the results of prenatal developmental toxicity or multigeneration studies were present in the Fraunhofer database on Fertility and Developmental Toxicity in experimental animals (FeDTex) database. Likewise, we evaluated 220 chemicals which had been tested in reporter gene assays on endocrine ((anti)estrogenic and (anti)androgenic) properties in the CALUX(®) test battery. There was a large spread of effect levels for substances within the chemical structure groups for both, in vivo and in vitro results. The groups of highest concern (diphenyl derivatives, planar conjugated systems with fused rings, phenols and organophosphates) correlated quite well, however, between the in vivo and in vitro data on estrogenic activity. For the 56 chemicals represented in both databases, lowest effect doses in vivo correlated well with the estrogenic activity in vitro. These results suggest that a panel of assays covering relevant AOPs and data on metabolism and toxicokinetics may allow prediction of relative reproductive or development toxicity potency within the identified chemical structure groups.
Geertje Lewin, Sylvia E Escher, Bart van der Burg, Nelly Simetska, Inge Mangelsdorf

2342 related Products with: Structural features of endocrine active chemicals--A comparison of in vivo and in vitro data.

48 samples50 ug300 units96 tests1600

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#23045189   2012/10/08 To Up

Testosterone treatment improves metabolic syndrome-induced adipose tissue derangements.

We recently demonstrated that testosterone dosing ameliorated the metabolic profile and reduced visceral adipose tissue (VAT) in a high-fat diet (HFD)-induced rabbit model of metabolic syndrome (MetS). We studied the effects of HFD and in vivo testosterone dosing on VAT function and the adipogenic capacity of rabbit preadipocytes isolated from VAT of regular diet (RD), HFD, and testosterone-treated HFD rabbits. VAT was studied by immunohistochemistry, western blot, and RT-PCR. Isolated rPADs were exposed to adipocyte differentiating mixture (DIM) to evaluate adipogenic potential. Adipocyte size was significantly increased in HFD VAT compared with RD, indicating adipocyte dysfunction, which was normalized by testosterone dosing. Accordingly, perilipin, an anti-lipolytic protein, was significantly increased in HFD VAT, when compared with other groups. HFD VAT was hypoxic, while testosterone dosing normalized VAT oxygenation. In VAT, androgen receptor expression was positively associated with mRNA expression of GLUT4 (SLC2A4) (insulin-regulated glucose transporter) and STAMP2 (STEAP4) (androgen-dependent gene required for insulin signaling). In testosterone-treated HFD VAT, STAMP2 mRNA was significantly increased when compared with the other groups. Moreover, GLUT4 membrane translocation was significantly reduced in HFD VAT, compared with RD, and increased by testosterone. In DIM-exposed preadipocytes from HFD, triglyceride accumulation, adipocyte-specific genes, insulin-stimulated triglyceride synthesis, glucose uptake, and GLUT4 membrane translocation were reduced compared with preadipocytes from RD and normalized by in vivo testosterone dosing. In conclusion, testosterone dosing in a MetS animal model positively affects VAT functions. This could reflect the ability of testosterone in restoring insulin sensitivity in VAT, thus counteracting metabolic alterations.
Elena Maneschi, Annamaria Morelli, Sandra Filippi, Ilaria Cellai, Paolo Comeglio, Benedetta Mazzanti, Tommaso Mello, Alessandra Calcagno, Erica Sarchielli, Linda Vignozzi, Farid Saad, Roberto Vettor, Gabriella B Vannelli, Mario Maggi

2942 related Products with: Testosterone treatment improves metabolic syndrome-induced adipose tissue derangements.

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#22791158   // To Up

The novel non-steroidal selective androgen receptor modulator S-101479 has additive effects with bisphosphonate, selective estrogen receptor modulator, and parathyroid hormone on the bones of osteoporotic female rats.

We have studied non-steroidal selective androgen receptor modulators (SARMs) to develop anti-osteoporosis drugs for males and females. Many SARMs have been studied for their anabolic effects on bone or muscle with reduced virilizing effects in male animals. However, the tissue selectivities of these agents in female animals have not been fully evaluated. We evaluated the novel SARM S-101479 from tetrahydroquinoline libraries in ovariectomized (OVX) rats. S-101479 preferentially bound to the androgen receptor with nanomolar affinity among nuclear receptors. It increased the bone mineral density (BMD) of femurs and diminished the effects on the uterus and clitoral gland in OVX rats. We then compared the effect of S-101479 on bone with those of commercial anti-osteoporosis drugs such as alendronate, raloxifene, and teriparatide. Furthermore, we evaluated the effects of combination treatments with these agents in OVX rats. After 16-week treatment, all agents significantly increased BMD, but the magnitude of bone mineral content (BMC) and/or bone size (projected bone area) were different. Alendronate, raloxifene, and teriparatide maintained BMC and bone size in this experimental dose. Only S-101479 increased BMC with bone size on single treatments. In combination treatment, S-101479 significantly increased BMC and bone size compared with single treatments of other agents. S-101479, like natural androgen, may have showed periosteal bone formation of the cortical area and indicated additive effects with commercial anti-osteoporosis drugs. These results indicate that S-101479 may be a useful anti-osteoporosis drug, particularly for patients with established severe osteoporosis.
Kazuyuki Furuya, Noriko Yamamoto, Yuki Ohyabu, Akito Makino, Teruyuki Morikyu, Hirohide Ishige, Kazuya Kuzutani, Yasuhisa Endo

1486 related Products with: The novel non-steroidal selective androgen receptor modulator S-101479 has additive effects with bisphosphonate, selective estrogen receptor modulator, and parathyroid hormone on the bones of osteoporotic female rats.

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#22597534   2012/05/17 To Up

Dihydrotestosterone inhibits lectin-like oxidized-LDL receptor-1 expression in aortic endothelial cells via a NF-κB/AP-1-mediated mechanism.

The mechanisms involved in the antiatherosclerotic effects of androgens are unclear. Although lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1) in endothelial cells plays critical roles in atherosclerosis, the effects of androgens on endothelial LOX-1 expression has not been examined. Therefore, to investigate the effects of dihydrotestosterone (DHT) on LOX-1 expression in rabbit aortic endothelial cells and cultured human aortic endothelial cells (HAEC), pellets containing DHT or placebo were s.c. implanted into 26 male New Zealand white rabbits at the time of castration or sham operation. The rabbits were then fed a high-cholesterol diet (HCD) for 2 wk. Microscopic examination of the aortic arch revealed that DHT significantly reduced HCD-induced LOX-1 expression in endothelial cells compared with placebo. In cultured HAEC, DHT at concentrations above 10(-9) to 10(-7) mol/liter inhibited TNFα-induced LOX-1 mRNA and protein expression. Deletion and mutation analysis of human LOX-1 promoter-luciferase constructs transfected into HAEC with an androgen receptor (AR) expression plasmid revealed that the 12-O-tetradecanoylphorbol-13-acetate (TPA) response element (TRE; nucleotides -60/-53) contributed to the inhibitory effects of DHT on TNFα-induced LOX-1 expression. Chromatin immunoprecipitation (ChIP) and re-ChIP assays revealed that TNFα- and TPA-dependent enrichment of p65 and phosphorylated c-Jun in the TRE chromatin region was inhibited by DHT-AR. Consistent with these results, DHT also suppressed TPA-induced expression of LOX-1. In conclusion, DHT exerts antiatherosclerotic effects by suppressing endothelial LOX-1 expression. This effect is partly mediated by the suppression of nuclear factor-κB- and activator protein 1-dependent activation of the LOX-1 promoter.
Yang Qiu, Tomoko Tanaka, Hajime Nawata, Toshihiko Yanase

1775 related Products with: Dihydrotestosterone inhibits lectin-like oxidized-LDL receptor-1 expression in aortic endothelial cells via a NF-κB/AP-1-mediated mechanism.

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