Formestane - CAS 566-48-3
Catalog number: 566-48-3
Category: Inhibitor
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Formestane is a second generation selective aromatase inhibitor with an IC50 of 80 nM.
CGP32349; CGP 32349; CGP-32349; 4OHA; 4OHAD; Formestane; Lentaron. NSC 282175; NSC282175; NSC-282175
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1.Role of Steroids in Hyperexcitatory Adverse and Anesthetic Effects of Sevoflurane in Neonatal Rats.
Zhang J1, Xu C, Puentes DL, Seubert CN, Gravenstein N, Martynyuk AE. Neuroendocrinology. 2015 Jul 1. [Epub ahead of print]
Recent studies have demonstrated that long-term developmental effects of neonatal anesthesia were more prominent in males. We tested whether steroids, in general, and sex steroids, in particular, are involved in the mediation of sevoflurane-caused paradoxical cortical seizures during the early postnatal period.
2.Studies on the minor metabolite 6a-hydroxy-androstenedione for doping control purposes and its contribution to the steroid profile.
Polet M1, Van Renterghem P, Van Gansbeke W, Van Eenoo P. Drug Test Anal. 2014 Oct;6(10):978-84. doi: 10.1002/dta.1618. Epub 2014 Feb 11.
Recent publications have shown that the concentrations of minor metabolites such as formestane and 6a-hydroxy-androstenedione (6aOHADION) are import parameters, capable of increasing the specificity and efficiency of steroid abuse screening. The importance of such minor metabolites has been recognized for some time, but setting up concentration thresholds is not that straightforward with a single quadrupole gas chromatograph mass spectrometer (GC-MS) because of the low concentrations; this is especially the case for 6aOH-ADION. The main aim of this study was to propose a concentration threshold above which the detected 6aOH-ADION is considered suspicious and isotope ratio mass spectrometry (IRMS) is recommended. Routine doping control samples (2128) from athletes that entered our lab and were not found suspicious for the intake of any doping substance were used to determine the baseline concentrations of 6a-OH-ADION. For this purpose, the more sensitive gas chromatography-tandem mass spectrometry (GC-MS/MS) was used, capable of quantifying these low concentrations with high reliability.
3.Mechanisms by which neonatal testosterone exposure mediates sex differences in impulsivity in prepubertal rats.
Bayless DW1, Darling JS, Daniel JM. Horm Behav. 2013 Nov;64(5):764-9. doi: 10.1016/j.yhbeh.2013.10.003. Epub 2013 Oct 11.
Neonatal testosterone, either acting directly or through its conversion to estradiol, can exert organizational effects on the brain and behavior. The goal of the current study was to examine sex differences and determine the role of neonatal testosterone on prefrontal cortex-dependent impulsive choice behavior in prepubertal rats. Male and female prepubertal rats were tested on the delay-based impulsive choice task. Impulsive choice was defined as choosing an immediate small food reward over a delayed large reward. In a first experiment to examine sex differences, males made significantly more impulsive choices than did females. In a second experiment to examine the organizational effects of testosterone, females treated with neonatal testosterone made significantly more impulsive choices than did control females and their performance was indistinguishable from that of control males. In a third experiment to determine if the effect of testosterone on performance is due to the actions of androgens or estrogens through its conversion to estradiol, males treated neonatally with the aromatase inhibitor formestane, which blocks the conversion of testosterone to estradiol, females treated neonatally with the non-aromatizable androgen dihydrotestosterone, and females treated neonatally with estradiol made significantly more impulsive choices than did control females and their performance was indistinguishable from that of control males.
4.Possible role of nitric oxide (NO) in the regulation of gender related differences in stress induced anxiogenesis in rats.
Chakraborti A1, Gulati K2, Ray A1. Nitric Oxide. 2014 Dec 1;43:74-80. doi: 10.1016/j.niox.2014.08.005. Epub 2014 Aug 28.
Gender related differences in stress induced neurobehavioral disorders have been reported although the mechanisms involved are not yet clear. The present study investigated the role of nitric oxide, an important biomodulator in the sex related differences in stress induced anxiety like behavior in rats. Restraint stress (RS for 1 h) was used as the experimental stressor and the effects of NO modulators were assessed in the elevated plus maze (EPM) test in both male and female rats. No metabolites (NOx) and asymmetric dimethyl arginine (ADMA) were measured in brain homogenates of these rats for corroborative purposes. RS induced anxiogenesis in both male and female rats and such changes were greater in males as compared to females. The behavioral alterations were associated with enhanced levels of ADMA and reductions in levels of NOx in brain homogenates - the effects being greater in intensity in males as compared to females. Pretreatment with NO precursor L-arginine (500 mg/kg) reversed the RS induced behavioral and biochemical changes, while NO synthase inhibitor L-NAME (50 mg/kg) had opposite effects.
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