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New SARM SR9011 available

SARMs, SARMs online shop

We have added new SARM SR9011 to our product list.

SR9011 is a novel circadian clock amplifier not yet tested in humans but is already a suspected performance enhancing agent. In mice, it has reduced blood fat and sugar levels while it increased energy expenditure and appetite. SR9011 had mild or nightlong interaction with wakefulness depending on light conditions, has anti-inflammatory properties and does not have overt toxicity. In a few cell lines it did not interfere with proliferation of normal cell lines specifically. Hence, Rev-ErbA? agonists, as shown by at least four lines of evidence, seem to have a broad spectrum of effects.

Read more about SR9011 or buy SR9011 in our store.

How does yohimbine interact with caffeine?

Nootropics

In 1989 there was a study that investigated the behavior of animals. Caffeine was anxiogenic in the context of exploration and social interaction while yohimbine was anxiogenic in the context of exploration but displayed anti-conflict properties in social interaction [1]. Unexpectedly, caffeine and yohimbine cancelled each others’ effects out.

An interesting study investigated rat vocalizations under the influence of either caffeine, yohimbine or amphetamine. 22 kHz sounds were interpreted as signals of alarm or distress while 50 kHz voice were interpreted as response to rewarding stimuli while mentioning that it is unknown whether the same signal is associated with anxiety [2]. Caffeine and amphetamine increased 50 kHz calls, yohimbine did not. In addition, it was shown that while caffeine and amphetamine were locomotor stimulants, yohimbine was not.

Yohimbine can promote fat loss by mildly increasing lipolysis when not counteracted by eating because after a meal the lipolysis-enhancement does not work [3]. In lower doses it does not increase blood pressure, heart rate or cause anxiety as much as ephedrine but larger doses have both cardiovascular and anxiogenic effects.

A human cardiology study [4]investigated caffeine, ephedrine and yohimbine in obese women during exercise (handgrip and cycloergometer). Caffeine and ephedrine increased heart ejection fraction during cycling (amount of blood pumped out of left ventricle, an increase may be considered usually beneficial) and did not alter the hemodynamics while resting. Addition of yohimbine increased diastolic blood pressure (that may be considered quite undesirable in this context) and heart rate (same interpretation) but decreased ejection fraction (same interpetation) and stroke index during rest (same interpretation). During exercise, yohimbine decreased ejection fraction during both exercises and increased cardiac load during exercise.

 

Bottom line: while yohimbine seems useful for fasted long-duration low-intensity fat burning training, it seems that combining it with substantial amounts of caffeine may be asking for trouble. Most importantly, yohimbine seems a very unwise choice for hard exercise (weightlifting, sprint, high-intensity interval training, intense cardio, and, if I may suggest, also pushing the limits with rough sex).

[1] https://www.ncbi.nlm.nih.gov/pubmed/2707309
[2] https://www.ncbi.nlm.nih.gov/pubmed/29909426
[3] https://www.ncbi.nlm.nih.gov/pubmed/12323115
[4] https://www.ncbi.nlm.nih.gov/pubmed/9545623

Effects and adverse effects of ibutamoren

SARMs

Ibutamoren (MK-677) has been researched with aims of increasing muscle mass, improving healing of injures and increasing quality of sleep. But there are also some side-effects related to blood pressure.

Growth hormone deficiency, if present, is associated with lower blood pressure independent of the time of the day [1] with normal response to exercise in humans. In rats whose hypophysis (part of brain that produces growth hormone) was removed, growth hormone lowered blood pressure, instead [2]. Mechanistically, alterations of growth hormone level may modify the blood pressure indeed but the exact dose relationship is unknown, and human studies must be considered more informative.

Growth hormone release amplifier MK-677 or ibutamoren is also relevant from the perspective of cardiovascular health: a study with obese humans has shown that ibutamoren moderately but significantly increased both diastolic blood pressure (mean 84 vs 79) and heart rate (mean 61 vs 56) [3]. In the first administration of ibutamoren, a transient elevation of prolactin and cortisol was observed, while the long term result was increase of fat free mass[4]. On the other hand, ibutamoren moderately decreased glucose tolerance in the long term, which reduces its potential utility for diabetic (as indicated by elevated glucose levels and glucose intolerance) and pre-diabetic (as indicated by elevated glycosylated hemoglobin levels in blood) humans. The effects of ibutamoren may be dependent on age and duration of administration. The negative effects may be more prominent in the elderly, as it was associated with congestive heart failure and elevated blood pressure in a study of elderly patients with hip fracture [4]. While there were some improvements in the gait speed and prevention of falling, the study was terminated early due to this side effect.

[1] https://www.ncbi.nlm.nih.gov/pubmed/11282052
[2] https://www.ncbi.nlm.nih.gov/pubmed/15525587
[3] https://academic.oup.com/jcem/article/83/2/362/2865156
[4] https://www.ncbi.nlm.nih.gov/pubmed/21067829

SARMs overview 2018 – 2019

SARMs

There were 135 PubMed-indexed Studies about SARMs (steroid androgen receptor modulators) at the end of January 2019.

SARMs were a hot topic in American Society of Bone and Mineral Research conference held in Quebec, Canada. The established technologies for improvement of bone function are high dose vitamin D, bisphosphonate drugs and somewhat more novel combination therapy of monoclonal antibodies that attack osteoclasts (cells that normally remodel the bone but cause osteoporosis if their proportion is out of balance) and recombinant parathyroid hormone that supports osteoblasts (bone-building cells) if used intermittently [1]. However, the SARMs were the most interesting from the novelty perspective.

A really interesting study published in 2019 discusses a SARM found from the nature (wild bitter gourd extract) and compared the SARM with testosterone in castrated mice (to unmask the effects of treatment from endogenous male steroid hormones). While testosterone increased the mass of both muscles and male accessory glands (prostate and seminal vesicles), the bitter gourd extract increased grip strenth and acrobatic/balance performance measured with as measured by the typical rotarod test [2]. Boosting mitochondria and their oxidative capacity as well as negating castration-induced muscle decline was proposed as mechanism of action.

A review paper was also published in 2019. It is somewhat a non-news that no SARMs are available as prescription drugs. In summary, the research has found that these molecules seem to have few if any drug interactions and the clinical studies suggest potential future applications for pathological muscle loss, benign prostate hyperplasia (BPH), hypogonadism and breast cancer [3] as well as, possibly, Duchenne muscular dystrophy (a disease which causes progressive weakness of muscles that is eventually lethal due to withering of breathing muscles). In contrast to uses related to disease, the use of SARMs as performance-enhancing agents was briefly discussed, as these drugs have anabolic effects with less side effects (without excluding potential for abuse), that make SARMs interesting for bodybuilding community.

In addition to regular additions to the set of studies dedicated to development of methods of doping detection, a few other studies were published in 2018: development of transdermal system of administration of SARM LY305 [4] – it improved the speed of muscle and bone repair without overt adverse effects in laboratory rodents, and was well-tolerated in human volunteers. Another study discovered that SARM S42 inhibited proliferation of prostate cancer cell line PC-3 [5]. Third study, expectedly, found that YK11 supported the function and proliferation of bone-building osteoblast cells of mice [6], and another study weighed in additional evidence by showing the anti-osteoporosis effects for the currently perhaps the best-known SARM ostarine [7].

Animal studies (especially optimistic ones for the sake of caution) must be taken with a grain of salt, though. A study found that LGD-4033 (that may also be known as ligandrol) metabolizes moderately differently in humans and horses, which adds a layer of complexity to interpretation of animal studies in general as well as doping detection in different species specifically [8].

While the aim of this text was to summarize the studies published in 2019 and 2018, a few studies of interest were published in 2017 deserve mentioning. We will cover this in future posts.

[1] https://www.ncbi.nlm.nih.gov/pubmed/30590370
[2] https://www.ncbi.nlm.nih.gov/pubmed/30600821
[3] https://www.ncbi.nlm.nih.gov/pubmed/30503797
[4] https://www.ncbi.nlm.nih.gov/pubmed/29527831
[5] https://www.ncbi.nlm.nih.gov/pubmed/29444261
[6] https://www.ncbi.nlm.nih.gov/pubmed/29491216
[7] https://www.ncbi.nlm.nih.gov/pubmed/29785666
[8] https://www.ncbi.nlm.nih.gov/pubmed/29334634

What to to against low testosterone – Replacement, SERMs, SARMs or something else?

SARMs

There’s a new review paper on an interesting topic, titled “Novel Therapy for Male Hypogonadism” from Miami University. We are let known that the last author of the paper [1] was the lead investigator of a drug trial in the past (Natesto, a formulation of testosterone for hypogonadism). The researchers are from Miami. Whether its tropical climate and beautiful beaches play a role on choice of the topic, remains unknown.

Word ‘hypogonadism’ comes from Ancient Greek – hypo meaning sub-; gonad meening seed seed). Hypogonadism is a clinical entity diagnosed with repeated measurement of low testosterone. Clinically, age-related hypogonadism is a type of sexual development delay in boys. Late-onset of hypogonadism can resemble some aspects of old age that are not liked very much by older men.

The paper discusses the recent papers on the clinical meaning of hypogonadism: one of the key issues is that older men with the hypogonadism complaints do not have low testosterone and vice versa.

Several treatment options are available. In addition to physical activity and lifestyle modification that is very important for late-onset hypogonadism, testosterone replacement treatment is the approved treatment while several experimental treatment options have been used as off-label treatments or in scientific studies.

Testosterone replacement is effective against hypogonadism symptoms, but is likely to adversely affect endogenous testosterone production and fertility parameters.

Selective estrogen receptor modulators (SERMs) have different estrogenic and antiestrogenic activity. SERMs such as tamoxifen and clomiphene improve serum lipids and bone density but tend to increase the incidence of venous thrombembolia. A SERM, Clomiphene citrate works by reducing negative feedback from estradiol to hypothalamus that is at the top of cascade leading to testosterone production. Clomiphene is quite widely used by doctors despite indication being off-label. Clomiphene raises rather than suppresses endogenous testosterone, and spares fertility, and the cost to the patient is lower.

Aromatase inhibitors such as anastrozole and exemestane work by reducing conversion of testosterone to estradiol. Estradiol in low doses has beneficial effects but increased levels of estradiol cause undesirable effects other than negative feedback to hypothalamus as well that can be summarized as feminization. While clomiphene is better at increasing testosterone concentration, aromatase inhibitor anastrozole was better at increasing testosterone : estradiol ratio.

Human chorionic gonadotropin (HCG) can raise endogenous testosterone production but also FSH is necessary for preservation of fertility. HCG has been used to treat azoospermia caused by steroid abuse. It may be combined with testosterone replacement to preserve the intratesticular levels of endogenous testosterone and and normal semen parameters.

Anabolic steroids such as nandrolone have also been revisited, lately, and considered as possibilities alternative to testosterone replacement because anabolic steroids have desirable effect of muscle selectivity

Finally, SARMs are considered as a novel option for testosterone replacement treatment. The selectivity of SARMs is more desirable than that of anabolic steroids, largely lacking androgenic activity in prostate or sebaceous glands, therefore making these compounds interesting for future pharmacy. However, as is often the case with novel substances – more research is needed before more widespread application may take place.

Source:
https://www.ncbi.nlm.nih.gov/pubmed/29886559

One may only wonder, which of the above would be the first to be considered as an alternative to testosterone replacement treatment first.

Using cryptocurrency to buy SARMs

SARMs online shop

Enhancetech accepts cryptocurrency payments. We support Bitcoin (BTC), Ethereum (ETH) and Bitcoin Cash (BCH).

Cryptocurrencies are getting more popular and many of our customers would like to use cryptocurrencies to pay for their orders. We are accepting main cryptocurrencies like Bitcoin, Ethereum and Bitcoin Cash. If needed we can accept also other common currencies like Litecoin, just let us know.

By using cryptocurrency to pay, we still need you to accept our sale terms. Please remember all our products, including SARMs, are for research use only.

 

 

New review for Unifiram

Nootropics

We have updated overview article of Unifiram. 

Unifiram (CAS# 272786-64-8) is a substance that was reported in year 2000 to have similar properties to piracetam but more potent in a mouse passive avoidance test. However, unifiram has shown pro-cognitive effects for mice by preventing amnesia induced by scopolamine (muscarinic antagonist), mecamylamine (nicotinic antagonist), baclofen (GABA-B agonist), clonidine (alpha-2 agonist), NBQX (AMPA antagonist) in passive avoidance test. Read more about Unifiram.

Unifiram is also available in our shop.

Effects of yohimbine to mind

Nootropics, SARMs

Yohimbine is usually considered an agent that helps to reduce body fat, increase sexual desire and ability for men as well as a stimulant that may cause unpleasant adverse effect of anxiety together with elevation of blood pressure.

However, according to the literature, yohimbine has some other effects as well, including effects on cognition, memory and sleep that may be of interest. Yohimbine (30 mg) reduced errors on letter flank test [1]. A simple version of letter flank test that shows ability to filter out irrelevant stimuli from detecting target letter is available online [2]. However, it increases rapid response impulsivity and errors in a somewhat more complex immediate memory test that has numbers instead of a single letter; the used dosage was a comparable 30 mg dose for a 75 kg person. The problem that occurred with yohimbine was that the test subjects did not read the number thoroughly and prematurely thought that the number was similar to another number presented just before the current. The test is explained online [4] but is not freely available.

Interestingly, yohimbine seems to have a truly interesting sex-specific effects on both memory and cognition of fear. Without affecting learning, it interrupted ability of women to generalize from learned memories [5]. Furthermore, the effect of yohimbine for processing fear-related signals (alteration of amygdala activity) is opposite for men and women [6].

A small study with medical students as subjects used a low dose. It was found that yohimbine improved following cognitive abilities: reaction time (single choice, not multiple choice), critical flicker fusion threshold and working memory (as measured by 1-back and 2-back tests) [7]. However, during glucocorticoid treatment or during high stress, yohimbine may be counterproductive for higher, flexible thought: yohimbine and cortisol together may reduce goal-directed behavior in favor of habitual behavior [8].

 

References:

[1] https://www.ncbi.nlm.nih.gov/pubmed/15858063
[2] https://www.psytoolkit.org/experiment-library/flanker.html
[3] https://www.ncbi.nlm.nih.gov/pubmed/15866563
[4] http://www.impulsivity.org/measurement/IMTDMT
[5] https://www.ncbi.nlm.nih.gov/pubmed/28253079
[6] https://www.ncbi.nlm.nih.gov/pubmed/23380165
[7] http://www.sciencedomain.org/abstract/7854
[8] https://www.ncbi.nlm.nih.gov/pubmed/22836250

Credit card payments and new batch of products

SARMs online shop

We have added credit card payments to Enhancetech web shop. Also there are new batch of products available.

Credit Card payments doesn’t include direct payments, but after checkout specific instructions will be sent. There is still option for SEPA payments, which means easy and quite fast bank transfers in EU countries.

There is also updates in our stock. Currently we are out of YK11, Ibutamoren and NSI-189, rest of the products are available for ordering.