Archive for December 2014

Raloxifen

Raloxifen

Raloxifen belongs to the class of compounds known as SERMs or selective estrogen receptor modulators. SERMs decrease activity of estrogen and are therefore considered an “anti-estrogen” treatment. However, SERMs do not act by decreasing serum estrogen or aromatase-mediated conversion, but rather through a blocking activity at the estrogen receptor on a cellular level. In other words, raloxifen and its metabolites are active at the estrogen receptor but not as an estrogen-like stimulus (agonist). Instead, they prevent estrogen from exerting its effects at the cellular level. This (as well as other means of blocking estrogenic activity or reducing estrogen levels) creates a rise in testosterone in men because testosterone production is modulated partially via serum estrogen levels.

Raloxifen and its sister drug tamoxifen are typically used in treating estrogen-receptor dependent breast cancer in women[1]. Raloxifen may prove to have more diverse uses than tamoxifen for several reasons:

Selective estrogen receptor modulators (SERMs) or estrogen agonists/antagonists have shown promise in osteoporosis in that they have the potential to reduce the risk of fracture, and also reduce the risk of breast cancer. SERMs maybe classified according to their core structure, which is typically a variation of the 17 beta-estradiol template and sub-classified according to the side chain at the helix 12 affector region. The best known are the triphenylethylenes such as tamoxifen, used in the management of breast cancer. However, the clinical application of this class of SERMs has been limited due to endometrial stimulation. A second class is the benzothiophenes such as raloxifene and arzoxifene, which have skeletal benefit with little, if any, uterine stimulation.[1]

In a study conducted by Christodoulakis et al, “raloxifene users did not exhibit any difference with respect to sex steroids and HOMA-IR levels.”[2]

Raloxifen increased serum testosterone but reduced serum IGF-1 in a study performed by Duschek et al:

In aging men serum levels of testosterone and insulin-like growth factor-1 (IGF-1) decline, potential factors in the reduced muscle strength, abdominal obesity, sexual dysfunction and impaired general well being of aging. The partial estrogen agonist and antagonist raloxifene increase serum testosterone levels in aging men, but the effect of raloxifene on serum IGF-1 levels in men is unknown. In this study the effects of raloxifene on IGF-1 levels and the associated increase in serum testosterone were compared to the effects of oral testosterone supplementation…. RESULTS: Compared to placebo raloxifene increased serum testosterone by 20% but it decreased serum IGF-1 levels by 24.5% (95% confidence interval (CI): -13.0 to -36.1%). No significant change in serum IGFBP-3 levels was found. The effect of raloxifene on serum IGF-1 has been observed with other oral estrogens, and, therefore, is likely to be ascribed to the partial estrogen agonist activity of raloxifene.[3]

According to Nordt et al, raloxifen may hold potential as an intervention in adolescent gynecomastia: “Newer treatment strategies, such as the antiestrogen raloxifene, have shown promising results; however, further studies are needed to determine long-term efficacy. As a result of the limited pharmaceutical treatment options, many more adolescents are seeking surgical intervention.[4]”

As the title of the study suggests, raloxifen is also a promising treatment for male osteoporosis:

Raloxifene has been shown to increase bone mineral density of the hip in men receiving androgen deprivation therapy for prostate cancer. Moreover, experimental data demonstrated dramatic increase in cell death in human prostate cancer cell lines after the treatment with raloxifene. All these observations suggest that SERMs may be useful for the prevention and treatment of osteoporosis not only in postmenopausal women but also in elderly men. However, our hypothesis should be tested in a proper designed clinical trial.[5]

Kastelan goes on to write that there are still issues of dose and duration to be assessed by further clinical study, as well as more markers of health and physical balance to be weighed against the benefits of raloxifen treatment.

More Peptide Info

Share with your friendsEmail this to someoneTweet about this on TwitterShare on Google+Share on FacebookPin on PinterestDigg thisShare on StumbleUponShare on TumblrShare on Reddit

CJC-1295 DAC

CJC-1295 DAC

CJC-1295 DAC has shown some amazing results as a growth hormone releasing hormone (GHRH) analog. Not only has CJC-1295 shown the ability to increase growth hormone and IGF-I secretion and its benefits, but it has been able to do so in very large amounts. Recent research studies have shown that CJC – 1295 stimulates GH and IGF-1 Secretion, and will keep a steady increase of HGH and IGF-1 with no increase in prolactin, leading to intense fat loss, and increases protein synthesis.

is a long acting Growth Hormone Releasing Hormone, which causes the anterior pituitary to release more growth hormone. GHRH is released in pulses in the body, which alternate with corresponding pulses of somatostatin (growth-hormone inhibiting-hormone). Clinical Research was first conducted for CJC-1295 during the mid-2000s. The objective of the peptide was to treat visceral fat deposits in obese AIDS patients, as increased levels of exogenous hgH are presumed to increase lipolysis (fat loss). The clinical research was ultimately successful for most research subjects. Ghrelin, released from the gut, which circulates and acts as a hunger hormone, has synergistic activity in the body with GHRH and also suppresses somatostatin to make way for the GHRH pulse. Studies shows that combining a GHRP-6 with CJC 1295 DAC, significantly increase the release of GH and IGF-1 production without an increase in prolactin. An example of a GHRP (GH Releasing Peptide) is Hexarelin or GHRP-2. CJC 1295 DAC is a exceptionally designed peptide and is known for being the finest of the hGH secretogues. The DAC (Drug Affinity Complex) portion increases the half-life by binding with serum albumin and protects the CJC-1295 DAC peptide from degradation. This was formed when a lysine link was bounded to DACs to a reactive chemical called maleimidoproprionic acid (MPA).

CJC-1295 DAC vs. CJC-1295 No DAC

CJC-1295 DAC and CJC-1295 (also known as Modified GRF 1-29) are both Growth Hormone Releasing Hormones (GHRH). Their action in the human body is identical but the difference between the two peptides are the span of the half-life. Modified GRF 1-29 and Sermorelin have a very short acting half-life of about 30 minutes, while CJC-1295 DAC has a half-life that can last up to approximately 8 days. Many a scientist have reported that the short half-life of Sermorelin and Modified GRF 1-29 is considered to be much more natural as they produce a short pulse of Human Growth Hormone.

ConjuChem and The Development of CJC-1295 DAC

CJC-1295 DAC is a tetra substituted peptide analogue of Growth Hormone Releasing Hormones with D-Ala, Gln, Ala, and Leu substitutions at positions 2, 8, 15, and 27 respectively. A Canadian biotechnology company called ConjuChem had invented CJC-1295. Clinical Research on CJC-1295 first began during the mid-2000s. The goal of the peptide, acting to raise hgh like Ipamorelin, was to treat visceral fat deposits in obese AIDS patients because it is presumed that increased levels of exogenous hGH increase fat loss, or lipolysis. In one study, results showed that the measured GH release in rats over a two hour period showed that CJC-1295 released twice as much GH as CJC-1293 DAC. This result makes it preferable for immediate effectiveness as a result of the longer peak. With the use of a Growth Hormone Releasing Peptide (GHRP), such as Growth Hormone Releasing Hexapeptide (GHRP-6) in conjunction with CJC-1295 DAC, a study has shown that the GHRP’s create a Growth Hormone pulse which helps the CJC-1295 work effectively. Clinical research’s involving CJC-1295 have shown that it had been successful for most research subjects..

More Peptide Info

Share with your friendsEmail this to someoneTweet about this on TwitterShare on Google+Share on FacebookPin on PinterestDigg thisShare on StumbleUponShare on TumblrShare on Reddit
eXTReMe Tracker