„Side effects” of some pharmaceuticals are researched as medicines against COVID-19

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Chemicals that are designed for one particular purpose can have unexpected side effects – often adverse, sometimes useful. For example, according to anecdotal evidence one of the SARMs (that is not even scientifically tested in humans) can tint the vision green or yellow. However, it is not the side effects of SARMs this post will be about. This post is about current coronavirus COVID-19 or SARS-2 (Severe Acute Respiratory Syndrome 2), a very close relative of coronavirus that caused SARS, and somewhat less close relative to very lethal MERS (Middle East Respiratory Syndrome) and research pertaining to possible treatment.

As concerns the coronaviruses, chemical informatics has revealed that a molecule that has been designed as a SERM (selective estrogen receptor modulator) could be repurposed as a medicine against novel coronavirus [1]. Of course, a computer analysis is not comparable to the rigour of actual human study but the model seems to be legit. Some other molecules found by informatics approach include emodin that has been found as a drug candidate in an earlier study [2]. Emodin is not a SARM, though, it is principally a a molecule that is responsible for laxative and estrogenic properties of certain medicinal rhubarb species. Of note, also melatonin was a „hit” in the analyses that matched coronavirus against the drug database. No experimental data on melatonin and coronavirus was found from scientific literature, though. Nevertheless, in the melatonin is considered as a potential treatment in another white paper [3] and one of the potential mechanisms might be that melatonin does not allow the COVID-19 to kill off the hosts’ T-cells so easily [4]. It seems likely that elderberries may have the same mechanism combating the upper respiratory tract viruses [5]. The other effect of melatonin that may facilitate the favourable income include protection from reactive nitrogen species. Indeed, in addition to direct antiviral mechanisms, immune stimulation and immune stimulant drugs [6] are also considered, and the most promising one, interferon beta-1 peptide is indeed a working solution against coronavirus, and included into medical guidelines [7]. It is known that lack of interferon beta is responsible for lethal pneumonia [8], which is the key difference between serious and non-serious coronavirus infections.

MERS (Middle East Respiratory Syndrome) coronavirus was tested against several drugs. In that study, a drug against malaria, chloroquine, and a drug against parasites, nitazoxanide, also had a „side effect” against the virus that caused MERS, and these two were more than order of magnitude more selective and potent (in vitro, at least) against MERS than most of the antiviral drugs that are used in the hospitals against COVID coronavirus now [9]. Lately, chloroquine has been added to several treatment guidelines, and the United Kingdom banned the export of chloroquine [10]. A now rather uncommon drug that was formerly used to treat arthritis, indomethacin was very effective in treating both SARS and dogs’ coronavirus in dogs [11] and there is an impressive list of potential molecules that could help against coronavirus in the very earliest research phase [12].

Finally, a list of food supplements has been published that has been suggested to ameliorate respiratory tract infections caused by RNA viruses such as influenza and coronavirus in general [13]:

Substance Dose
Ferulic acid 500-1000 mg
Lipoic acid 1200-1800 mg (in place of ferulic acid)
Spirulina 15 g (or 100 mg PCB)
N-Acetylcysteine 1200–1,800 mg
Selenium 50-100 mcg
Glucosamine 3,000 mg or more
Zinc 30-50 mg
Yeast Beta-Glucan 250-500 mg
Elderberry 600–1500 mg

[1] https://www.ncbi.nlm.nih.gov/pubmed/32194980
[3] https://www.sciencedirect.com/science/article/pii/S0024320520303313
[4] https://onlinelibrary.wiley.com/doi/full/10.1046/j.1600-079X.2003.00105.x
[5] https://www.ncbi.nlm.nih.gov/pubmed/31560964
[6] https://www.ncbi.nlm.nih.gov/pubmed/32205350
[7] https://www.ncbi.nlm.nih.gov/pubmed/32164424
[8] https://www.ncbi.nlm.nih.gov/pubmed/26867177
[9] https://www.nature.com/articles/s41422-020-0282-0
[10] https://www.gov.uk/government/publications/medicines-that-cannot-be-parallel-exported-from-the-uk
[11] https://www.ncbi.nlm.nih.gov/pubmed/17302372
[12] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4195804/
[13] https://www.ncbi.nlm.nih.gov/pubmed/32061635

Effects of Ibutamoren on brain

Nootropics, SARMs

It seems that short-term use of ibutamoren after short-term stress reduces anxiety while long-term use during chronic stress increases anxiety.  A new paper [1] describes a mechanism wherein a ghrelin mimetic (ibutamoren mesylate) can enhance fear learning in rats in the context of chronic stress. The said mechanism showed that a ghrelin agonist did not activate HPA stress axis, whose downstream effector hormone is cortisol. Ghrelin is a stress hormone by itself. Growth hormone receptors were up-regulated during repeated stressful events, ghrelin agonist increased growth hormone levels and the fear learning of the rats grew in response to growth hormone. The mechanism was confirmed by using ghrelin antagonist that blocked the enhanced fear learning. In case of the short time frame, the opposite seems to be true, as short time stress followed by ghrelin agonist reduces stress symptoms in mice [2]. Fourth study also demonstrated that ghrelin weakens fear learning in generally unstressed rodents while chronically stressed rats had elevated levels of hunger hormone and fear learning ended up with fewer ghrelin receptors. High expression of ghrelin receptors reduces anxiety [3], while low levels have the opposite effect. Hence, it seems that long-term ibutamoren may exacerbate long-term stress, and brain ghrelin receptor down-regulation is the probable explanation. It seems likely, that transient or occasional increases in ghrelin receptor activation (such as after interval exercise [4]) may be more adaptive than chronic elevation regime.

[1] https://www.nature.com/articles/mp2013135

[2] https://www.ncbi.nlm.nih.gov/pubmed/22521145

[3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4886665/

Get 10% off with cryptocurrency payout option

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We are offering extra 10% discount when paying for SARMs and Nootropics by cryptocurrency.

Discount appears in checkout, when choosing “Bitcoin or other cryptocurrency” payment method. We are providing this as as we don’t have to pay credit card charging fees or other type of fees. At the same time we are supporting philosophy behind the cryptocurrency.

We accept Bitcoin, Ethereum, Bitcoin cash. For other cryptocurrency, please contact us.

Please see our shop for all our provided products.

SARMs bans in China and USA

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In november 2019, USA started introducing SARMs control act that would make SARMs illegal to sell or possess but it has not become a law, yet (date: 02/14/2020) [1]. While China may have banned export of SARMs in the same time, several SARMs are bidded on alibaba.com [2]. In USA, the aim of SARMs ban is to protect the consumers from unscrupulous vendors that sell SARMs as food supplements as well as buyers that unknowingly buy food supplements unknowingly. On the other hand, it will also mean that selling and buying SARMs becomes criminal, even if these substances are considered as research chemicals by both parties.

The parties that support criminalization include entertainment sports industry, pharmaceutical industry and natural products industry: U.S. Anti-Doping Agency, the American Herbal Products Association, the Consumer Healthcare Products Association, the Council for Responsible Nutrition and the United Natural Products Alliance.

Enhancetech has most of the SARMs back in stock and there shouldn’t be any problem according to our manufacturer. We might not be able to ship to US, after SARMs control act would become a law. So we suggest all US customers to order SARMs as soon as possible.

[1] https://www.congress.gov/bill/116th-congress/senate-bill/2895
[2] www.alibaba.com
[3] https://www.grassley.senate.gov/news/news-releases/grassley-whitehouse-introduce-legislation-regulate-sarms

Summary of SARMs doses used in human studies

Nootropics, SARMs

Overview of SARMs dosages used in human studies.

SARM/Nootropic and dosage used:
Ostarine 3 mg [1]
Ligandrol 1 mg [2]
YK-11 Unknown
RAD120 Unknown
Cardarine Unknown
SR9009 Unknown
SR9011 Unknown
Unifiram Unknown
PRL-5-83 5 mg [3]
Yohimbine Usually 5…30 mg [4],[5]
Hordenine Unknown but present in beer 1…6 mg [6]
PEA Unknown but see [6],[7]

[1] https://www.ncbi.nlm.nih.gov/pubmed/27138015
[2] https://www.ncbi.nlm.nih.gov/pubmed/27138015
[3] https://www.ncbi.nlm.nih.gov/pubmed/?term=PRL-8-
[4]https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3430403
[5] https://www.ncbi.nlm.nih.gov/pubmed/9315493
[6] https://www.ncbi.nlm.nih.gov/pubmed/30409657
[7] https://www.ncbi.nlm.nih.gov/pubmed/26481102
[8] https://www.ncbi.nlm.nih.gov/pubmed/26481102

SR9009 (Stenabolic) now available

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We have added new SARM SR9009 to our provided products.

SR9009 also known as Stenabolic is an experimental circadian rhytm modulator (RevErb-alpha agonist). In one hand, SR9009 is said to be attractive as a performance-enhancing agent, yet, in the other hand, its use has been discouraged because it is potentially harmful. The desire to discourage its use has prompted development of its screening methods. So far, SR9009 has revealed anti-inflammatory properties (suppressing activation of several pro-inflammatory cytokines including tumor necrosis factor alfa, whose downstream effect was suppression of tumor necrosis factor alpha). The anti-inflammatory effects have been shown in animal models of endometriosis, heart attack, Alzheimer’s disease and some autoimmune diseases.

Read more about SR9009 or buy SR9009 in our store.

Cholesterol, Muscle Mass and SARMs

SARMs

Excessive blood cholesterol is considered an important risk factor of cardiovascular diseases. Excessive blood cholesterol has both genetic and dietary component. It is also known that cholesterol is either LDL (low density lipoprotein) HDL, also known as “good cholesterol” and “bad cholesterol”, respectively.

The non-pharmacological strategy to improve blood cholesterol is improving diet (broadly – less junk food and more salad) and exercise, which are aimed at lowering LDL without lowering HDL[1]. The most effective foods for lowering LDL are oatmeal, kidney beans, apples, pears, bananas, berries, fish, nuts, avocados, olive oil, and, good news for body builders, whey protein. On the other hand, dairy fats (cream, butter, cheese) and trans fats (crackers and cakes, especially the cheaper ones) raise the bad cholesterol [2]. Especially in overweight subjects, calorie restriction lowers increased cholesterol [3]. For high risk patients, statins are used. From the field of herbal medicine, several lines of evidence suggest that berberine works similarly well [4],[5] with the reservation that berberine research lacks the industry-supported large studies. Cocoa is a well-researched food, and while chocolate is suspicious due to huge sugar content, cocoa supplements significantly improve the metabolic profile as well [6]. Of research chemicals, cardarine has been one of the more promising substances: while the research of the substance has been abandoned by the industry, it is used for research. While the original effects revealed very specific effect of raising good cholesterol in very low doses and lowering bad cholesterol in higher doses, later research has revealed that it counteracts especially bad, endothelium-damaging form of cholesterol called oxLDL [7].

Exercise program of older men showed that after a year or half, there were no improvements in grip strength, body mass index or bad cholesterol but there were improvements in body shape, walking speed, one leg standing and good cholesterol [8]. On the other hand, in children a rather intriguing counter-intuitive association was found: fatter children had more good cholesterol [9]. In addition, higher muscle mass may lower cardiovascular risks for boys only [10]. However, the good news is that for older folks, even two strength training sessions per week helped to lower cardiovascular risks, especially in case of higher blood pressure and elevated cardiovascular inflammation marker hsCRP[11]. Research suggests that for adults, both men and women, hand grip strength (relative to body mass) and relative fat mass (fat mass index) may be the best independent predictors of cardiovascular health [12].

SARMs are double edged swords. In one hand, SARMS seem to have good safety combined with beneficial effects on muscle and bone, they have some drawbacks similar to steroids: SARMS lower good cholesterol significantly and dose-dependently according to multiple studies [13],[14],[15],[16]. The effects of androgens on blood profile are not just negative because the triglyceride levels tend to be improved. A monkey study of a novel dermally administered SARM that demonstrated increased muscle mass without lowering good cholesterol by reducing exposure of liver to that SARM, and a SARM that atypically did not lower good cholesterol have been revealed in clinical human studies, as well [Ahv],[Ahv+1].

Time will tell whether newer SARMs will have the same benefits as those that have been investigated for a longer time (i.e. ostarine) without having the drawback of lowering the good cholesterol. The research is improtant, because the effects seem really interesting for older people especially, and the proportion of older people is increasing proportionally almost worldwide.

[1] https://www.ncbi.nlm.nih.gov/pubmed/30953636
[2]https://www.mayoclinic.org/diseases-conditions/high-blood-cholesterol/in-depth/cholesterol/art-20045192
[3] https://www.ncbi.nlm.nih.gov/pubmed/31252598
[4] https://www.ncbi.nlm.nih.gov/pubmed/26520899
[5] https://www.ncbi.nlm.nih.gov/pubmed/31094214
[6] https://www.ncbi.nlm.nih.gov/pubmed/31056655
[7] https://www.ncbi.nlm.nih.gov/pubmed/27573670
[8] https://www.ncbi.nlm.nih.gov/pubmed/31111014
[9] https://www.liebertpub.com/doi/full/10.1089/chi.2019.0122
[10] https://www.ncbi.nlm.nih.gov/pubmed/30813304
[11] https://www.ncbi.nlm.nih.gov/pubmed/30774600
[12] https://www.ncbi.nlm.nih.gov/pubmed/30424569
[13] https://www.ncbi.nlm.nih.gov/pubmed/28449232
[14] https://onlinelibrary.wiley.com/doi/full/10.1007/s13539-011-0034-6
[15] https://www.ncbi.nlm.nih.gov/pubmed/22459616
[16] http://www.jbc.org/content/285/22/17054.full
[17] https://www.ncbi.nlm.nih.gov/pubmed/26683992
[18] https://www.ncbi.nlm.nih.gov/pubmed/29527831

Witch hunt against performance-enhancing drug users

SARMs

“Was the government to prescribe to us our medicine and diet, our bodies would be in such keeping as our souls are now.” — Thomas Jefferson

While it is understandable that competitive sports event organizers want to keep their events clear from the performance-enhancing drugs due to their values, the aim to extend that policy to laymen with a threat of a felony level (sic!) criminal offense seems clearly less justified both economically and morally. It can be reasoned that punitive laws are not in the interest of taxpayers. Average cost of per recruit in a cohort study is about ten dollars for offline recruitment and the cost can be further reduced by a third if online recruitment methods such as Facebook are used [1]. On the other hand, cost per year spent in prison is at least 30 000 dollars [2]. It would be more reasonable and cheaper to label the the said performance-enhancing drug users as “test subjects” and investigate them than label the said experimenters as “offenders” and put them into the jail. If the nonmedical use of substances could be epidemiologically monitored with compulsory following of a study protocol, then it should satisfy both moderate authoritarians and libertarians. If the use of SARMs is positioned clearly as that of performance-enhancement rather than that of medical, it should unburden medical and pharmaceutical regulatory authorities from some of the responsibility. On the other hand, it would position the sports authorities as major stakeholder, as seems to be the case (pharmaceutical industry does not seem to be major stakeholder because use of SARMs is not at odds with their major economic interests). In order to draw the boundaries that would allow the laypersons to use SARMs, the concerns of sports authorities must be taken into the account, and We suggest that science would be perfect arbiter while observation with the right to cancel the study due to health concerns is not sufficient means of regulation.

[1] https://www.ncbi.nlm.nih.gov/pubmed/28249833
[2]https://www.marketplace.org/2017/05/19/how-much-does-it-cost-send-someone-prison/

The Proposed SARMs Control Act

SARMs

There is new bill in Congress that would ban SARMs. Should possession of SARMs become a dangerous criminal act then? 

United States senators are pushing a bill that would reclassify SARMs as illegal substances (Schedule III) that would be treated similarly with anabolic steroids and some other drugs such as ketamine or buprenorphine. The parties that are interested in banning SARMs in USA are US Anti-Doping Agency, Council for Responsible Nutrition and Federal Law Enforcement Officers Association. While it is already clear that FDA has not approved SARMs as pharmaceuticals, the parties that are interested in enacting punitive laws pertinent to SARMs capitalize on possible negative health consequences. On the other side of the coin, a more plausibly benevolent argument is that under the less strict laws it is more difficult to stop the unscrupulous vendors who include SARMs as unlisted ingredients in their “food supplements”, which has been the concern of Council of Responsible Nutrition. Without saying, such cheating of consumers is already illegal. The bill aimed at making possession of a SARM a felony did not pass in April 24, 2018 [1]. What are the probable implications of this bill passing? “Once that happens, state and local police can arrest for SARMs, so that possessors are only one unexpected car stop or one bitter ex-spouse phone call away from a set of handcuffs.”[2].

[1] https://www.govtrack.us/congress/bills/115/s2742
[2] https://www.steroidlaw.com/2019/01/the-proposed-sarms-control-act/

New SARM SR9011 available

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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.