# Liquidex and the many possible applications of this highly effective AI



## CEM Store (Oct 2, 2013)

*The Basics:*
Anastrozole (Liquidex or Dex) is a non-steroidal aromatase-inhibiting compound in the class of compounds known as aromatase inhibitors (AI's). Liquidex inhibits the synthesis of estrogen. It does so by binding reversibly to the aromatase enzyme which is responsible for the production of estrogen.  Aromatase is the enzyme that catalyzes the conversion of androgens into estrogens.  Liquidex works through competitive inhibition for the aromatase enzyme and inhibits the conversion of androgens to estrogens in peripheral tissues outside the CNS as well as a few CNS sites in various regions within the brain.

The research of the inhibition of aromatase is important in many types of research. One of these types of research is cancer research, this is because scientists have found that some types of cancer growth are increased by the presence of the hormone estrogen. This is because sex hormones such as estrogen can cause hyperplasia in tissues. Liquidex has been found to work very well at inhibiting the synthesis of estrogen which has led to its extensive use in cancer research as well as many other areas hormone related, which I will touch on in this article.

*Early Liquidex research:*
Early on in AI research the important regulatory actions of aromatase were found, acting in an autocrine, paracrine, intracrine, neurocrine, and juxtacrine way. This research also showed its organ specific effects regarding transcription. These early studies of aromatase and the ultimate utilization of AI's as highly effective tools for cancer and reproductive disorder research has greatly advanced our understanding of hormones, AI's and their role or possible application in many areas and functions of the body. At an early stage of Liquidex research, researchers recognized that inhibition of this enzyme could have major practical applications for a vast array of conditions. Some life threatening and others less serious to life, yet still worth researching such as the treatment benign disorders like Gynecomastia (Gyno). 

*Liquidex and Gyno:*
The condition "Gyno" is typically be a result from imbalances between estrogen and androgen concentrations in the body of male animals. Although Gyno is a benign disorder and not of immediate health risk, it can still have devastating effects in the males of various species. With extremely abnormal and excessive breast growth it may damage the chances of reproduction and interaction with potential mates within the species. This can affect the number of new births as well as the overall quality of life for the animal with the Gyno condition. This is why Gyno research is still very important in my opinion, even though it is seen as a nonlife threatening condition. The good news is Liquidex has been shown to be very a potent and effective AI for decreasing estrogen and even increasing testosterone concentrations! 

It was shown in research that Liquidex administration was well tolerated by research subjects and that it was also shown effective in subjects with an old pre-existing Gyno conditions. In subjects with more recent gyno Liquidex was shown to have a 50% or greater reduction in total breast volume by the end of the research experiments vs subjects with old pre-existing Gyno. This study I mention was done between a Liquidex and placebo control group for the assessment. Liquidex has a very positive outcome in its application for both old or new Gyno conditions alike, but for better research results in a study aimed at reversing Gyno it should be made note of the fact recently developed Gyno will react to treatment in research better than old Gyno.

Some may say "why not just cut the glands out and be done with it already"? Well Gyno has been traditionally treated with this type surgery (cutting out the glands/mass), but that may only cover up a possible underlying issue of hormonal dysfunction. 

Estrogen is not all just about Gyno, there are many other risks involved with having abnormally high estrogen. In a research study with Liquidex it was noted; "We report here our experience with two cases of gynecomastia who were successfully treated with the aromatase inhibitor anastrozole."  This is amazing news for researchers in the field of hormone research because in some if not many cases Gyno may not be the only cause for concern and simply taking out a gland (possible warning sign for hormonal dysfunction) is not be the best way to go about it. 

In more current Gyno research with Liquidex it was shown that Liquidex was rapidly absorbed orally and that it hit its maximum concentration in under 1 hour. It was also shown to have the added bonus of having a slow clearance time of; "1.54 liters/h and a terminal half-life of 46.8 h. Testosterone/estradiol ratios increased significantly with concomitant increase in LH/FSH concentrations indicating aromatase blockade." This is really good news because it calls for less frequent administration and more stable blood levels per administration. It was also shown to reduce breast size similar to earlier research (approximately 63%) and breast volume (approximately 57%) and as stated earlier the compound is well tolerated by research subjects.


*Liquidex, Cancer and estrogen effects:*
Another reason to keep estrogen levels within normal range in subjects with hormonal dysfunction is because it has been found that excess estradiol in can cause benign prostatic hyperplasia, Gyno (as already mentioned), and symptoms of hypogonadism. If that wasn't bad enough add on; an increased risk of stroke, heart attack, chronic inflammation, prostate enlargement and even possibly enhancing prostate cancer growth!   Keeping Estrogen in check is no joke and this is why its research is so important. Increasing evidence shows that estrogens also play a big role in lung cancer proliferation and progression. In a study done to determine if Liquidex would prevent the development of lung tumors induced by a tobacco carcinogen or in combination with the ER antagonist fulvestrant; "ovariectomized female mice received treatments with the tobacco carcinogen and Dex, results showed significantly fewer NNK-induced lung tumors (mean = 0.5) compared with placebo"  This is great news for those that have to do tobacco based research, be it the negative effects or ways to avoid the negative effects of tobacco. Liquidex can play a big role in that research area as well as many other cancers.

*Liquidex, the brain and other AI's:*
Research has shown that brain structures and functions are directly affected by hormones. A while back hormones were seen as compounds that were only related to reproductive functions and sexual phenotypes. This was not the case and we see this now with more advanced research into hormones and their many various actions in the body. 

In a recent research study on this subject it was shown that "ovariectomy trimmed the dendritic spines of female rat primary somatosensory cortical neurons and estradiol supplement reversed it". In another; "The brain distribution of nonsteroidal aromatase inhibitors was investigated in mice to understand their interactions with brain aromatase.- The brain-to-plasma ratio (Kp,brain , mL/g brain) of anastrozole was 0.0299 ? 0.0068, which was lower than that of letrozole (0.383 ? 0.048) and vorozole (0.185 ? 0.031) despite their similar physicochemical properties." This study clearly shows that not all AIs act in the same way, even though their intended purpose/function is the same and that Liquidex have an effect on the brain as well as the body.



*Liquidex and testosterone:*
In research using rat C6 glioma cells which are commonly used to research the functions of glial cells and to evaluate the presence of testosterone and its metabolism; "in rat C6 glioma cells, we cultured them in media with or without the addition of testosterone propionate and anastrozole, a blocker of aromatase, the enzyme needed to transform testosterone into estradiol. Confluent cells were exposed to the test media for 48 h and then collected. Cell pellets were used to determine testosterone by radioimmunoassay. The C6 cells contained detectable levels of testosterone and the levels increased with the addition of testosterone to the medium. Aromatase blockage by anastrozole increased cellular levels of testosterone regardless of the addition of exogenous testosterone." Showing us that testosterone is present in rat C6 glioma cells and that it can be metabolized by aromatase. This study also shows us that Dex has the ability to raise testosterone levels as well as lower estrogen levels. 

*AI's, SERMs and female research subjects:*
Liquidex has been shown to have a very positive effect on endometriosis conditions. Endometriosis is a gynecological condition in which cells from the lining of the uterus (endometrium) appear and grow outside the uterine cavity. In a study done with Liquidex on the growth of endometriotic like lesions in a murine model of endometriosis it was shown that cell proliferation was significantly diminished and apoptosis was significantly enhanced. Although Liquidex is an AI and a compound known as "Raloxifene" is a SERM, both were seen in research to have caused an equal regression of the experimental endometriosis that was statistically significant. 

This says to me that in some types of research a combination of compounds might be a better avenue for the most effective research outcome and we are happy to be able to offer you only the highest quality research compounds! Be it Ralox or Dex, our products will help you further your research into this very fascinating and expanding field of research. 

In a study with animals administered Liquidex vs. a control group not given Liquidex; "macroscopic changes of uterus and vagina were not found." Also noted in the study; "The values of absolute and relative wet weight of uterus and vagina in the groups ANA 0.05 and ANA 0.5 were comparable with the control. Histological examination did not show atrophic changes in endometrium of uterus and in epithelium of vagina in anastrozole-treated animals. In the group ANA 0.5 myometrium was significantly grosser than in the group ANA 0.05 (P<0.05). Anastrozole neither affects parameters of plasma lipid metabolism (triacylglycerols, total cholesterol, low - density lipoprotein cholesterol and high - density lipoprotein cholesterol) nor serum levels of sex hormones (estradiol, testosterone, dehydroepiandrosterone)."  This is a great finding showing just how safe Liquidex research can be for the subjects of the female gender. 
In a study done to compare the effects of anastrozole (AI), Letrozole (AI) and Tamoxifen (SERM) on induced pulmonary fibrosis; "Eighty female Wistar albino rats were divided into eight groups- tamoxifen group increased the radiation-induced pulmonary fibrosis (p = 0.005). However, using either anastrozole or letrozole with RT did not increase the radiation-induced pulmonary fibrosis (p values were 0.768 and 0.752, respectively)."  This shows that Liquidex may be a better option for some types of research and that the use of both Liquidex and letrozole appears to be safe with pulmonary fibrosis based research, without increasing the risk of pulmonary fibrosis in subjects.

*Liquidex, Estrogen, Diabetes and Reno-protective effects: *
Streptozotocin (STZ) induced diabetic rat exhibit a decreased circulating testosterone and increased estradiol levels. In a study done to examine whether inhibition of estradiol synthesis with Liquidex administration can prevent diabetes associated renal injury using male Sprague-Dawley nondiabetic, STZ-induced diabetic, and STZ-induced diabetic rats it was shown that blocking estradiol synthesis with Liquidex in STZ-induced diabetic rats is reno-protective! Administration of Liquidex reduced diabetes-associated increases in plasma estradiol by 39% and increased plasma testosterone levels by a whopping 187%! Who says hormones are only related to gender and sexual function? No one anymore I hope!


Liquidex really does has many areas of research worth pursuing and a vast array of possible applications.
Thank you for reading and I hope this has added to your understanding of Liquidex and all it can do for your research.

Check it out >> Liquidex


Ref:

1)	Alleviating anastrozole induced bone toxicity by selenium nanoparticles in SD rats Vekariya KK, Kaur J, Tikoo K. Alleviating anastrozole induced bone ... [Toxicol Appl Pharmacol. 2013] - PubMed - NCBI
2)	Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system.Miyajima M, Kusuhara H, Takahashi K, Takashima T, Hosoya T, Watanabe Y, Sugiyama Y. Investigation of the effect of active efflux at ... [J Pharm Sci. 2013] - PubMed - NCBI
3)	History of aromatase: saga of an important biological mediator and therapeutic target.Santen RJ, Brodie H, Simpson ER, Siiteri PK, Brodie A. History of aromatase: saga of an important biolog... [Endocr Rev. 2009] - PubMed - NCBI
4)	Side effects of anastrozole in the experimental pre-menopausal mammary carcinogenesis.Sadlonova V, Kubatka P, Kajo K, Ostatnikova D, Nosalova G, Adamicova K, Sadlonova J. Side effects of anastrozole in the experimental pr... [Neoplasma. 2009] - PubMed - NCBI
5)	Effects of morphine on testosterone levels in rat C6 glioma cells: modulation by anastrozole.Ceccarelli I, Rossi A, Maddalena M, Weber E, Aloisi AM. Effects of morphine on testosterone levels in... [J Cell Physiol. 2009] - PubMed - NCBI
6)	Comparison of the effects of aromatase inhibitors and tamoxifen on radiation-induced lung toxicity: results of an experimental study.Yavas G, Yavas C, Acar H, Toy H, Yuce D, Ata O. Comparison of the effects of aromatase i... [Support Care Cancer. 2013] - PubMed - NCBI
7)	Prevention of tobacco carcinogen-induced lung cancer in female mice using antiestrogens.Stabile LP, Rothstein ME, Cunningham DE, Land SR, Dacic S, Keohavong P, Siegfried JM. Prevention of tobacco carcinogen-induced lung... [Carcinogenesis. 2012] - PubMed - NCBI
8)	Inhibition of estradiol synthesis attenuates renal injury in male streptozotocin-induced diabetic rats.Manigrasso MB, Sawyer RT, Marbury DC, Flynn ER, Maric C. Inhibition of estradiol synthesis... [Am J Physiol Renal Physiol. 2011] - PubMed - NCBI
9)	Comparison of the effects of raloxifene and anastrozole on experimental endometriosis.Altintas D, Kokcu A, Kandemir B, Tosun M, Cetinkaya MB. Comparison of the effects o... [Eur J Obstet Gynecol Reprod Biol. 2010] - PubMed - NCBI


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