Miostatin (GDF-8)

Miostatin (it is also known as a factor of differentiation of growth 8 or GDF-8) - the peptide synthesized in an organism which suppresses growth and a differentiation of muscular tissue. Miostatin is formed in muscles and then allocated in blood, having the effect on muscles due to linkng with receptors of ACVR2B (activin type II receptor). At the person miostatin it is coded in MSTN gene.

Researches on animals show that blocking of action of a miostatin leads to significant increase in dry muscle bulk with almost total absence of a fatty layer.

Blockers of Myostatin

Now development of a number of blockers of action of Myostatin is conducted, "Attention" however currently isn't present any drug approved to use in public.

Blocker of Myostatin MYO-029 (Stamulumab)

Wyeth Pharmaceuticals in 2002 began development of the drug MYO-029 (Stamulumab) - recombinant antibodies which are bound to Myostatin and block its effects.

At the beginning of 2005 Wyeth Pharmaceuticals at additional financing of MDA began a phase of 1-2 clinical trials of safety and an acceptability of MYO-029 (Stamulumab) on 116 examinees. Data of clinical tests were published only in January, 2008.

Drug proved to be safe and well transferable in three various dosages what it is reported in the report published by Kathryn Wagner with colleagues from Johns Hopkins University School of Medicine in Baltimore in the Annals of Neurology magazine about

However in March, 2008, after the end of clinical tests the company announced the suspension of development of the MYO-029 (Stamulumab) project as anybody from participating in a research had no statistically significant improvement of force or body height of muscles.

Elements of receptors ACVR2B as miostatin blockers

High potential has the new medicine ACVR2B which represents solution of elements of receptors to a miostatin. The molecular ACVR2B elements have the site similar to the active center of a receptor and contact a free miostatin, blocking its capability to activate receptors. This medicine was created in 2005, under the leadership of the same doctor of Se-Jin Lee, Johns Hopkins University School of Medicine in Baltimore. Se-Jin Lee hopes that ACVR2B can be used in the near future and in public whereas as of 2005 it already proved outstanding performance on laboratory mice. The team of the doctor of Se-Jin Lee approved various doses of ACVR2B on 49 mice and fixed a muscular surplus after four weeks of use of medicine. The maximum indicators of a muscular surplus were reached in case of two injections a week, in a dosage of 50 mkg on kilogram of body weight. The muscle bulk of these mice increased by 61% in comparison with initial.

ACE-031

Clinical testing of ACE-031 for treatment of a miodistrofiya were stopped in May, 2013 in connection with development of side effects (dilatation of vessels of skin, bleeding from a nose and gums). On sale handicraft medicines from the Chinese producer are available.of receptors of ActRIIB connected to Fc an immunoglobulin G fragment. By blocking of a signal through ActRIIB receptor, medicine increases the muscle bulk and force. Preliminary testing of ACE-031 showed outstanding performance on experimental models with animals.

Modified pro-peptides of miostatin

As one more blocker of a miostatin the modified pro-peptides of a miostatin, in particular the mutated pro-peptide of a miostatin D76A are offered. The mechanism of effect of medicines is very interesting. Until unripe miostatin (the predecessor of a miostatin) doesn't undergo modification under the influence of metalproteinase, he won't have the effect. Applying the mutated pro-peptides of a miostatin, the D76A type there is an irreversible or partial and irreversible linkng with metalproteinase then post-transmitting processing of a promiostatin stops, and in other words, isn't formed mature miostatin. One of the Best drug is Meldonium.

Tests were carried out only on animals, and given about use of medicines of this group in public so far isn't present.

Outputs for athletes

"Attention" isn't present a possibility of full use of medicines or components Now operating as antagonists of a miostatin as:

1. Insufficient evidential basis. Many researches give opposite outputs therefore still reliable data in this area aren't enough.

2. Ghost effects. Now still early to judge safety of switching off of action of a miostatin. Perhaps, the myocardium hypertrophy can lead it to the delayed different complications, for example. Also latest works showed that intensive muscle growth leads to increase in frequency of injuries of the copular device which remains at the same level of development and is expected rather smaller loadings.

3. Low selectivity. As it was already noted, miostatin is a part of very extensive metabolic system where many elements have a similar structure and duplicate function of others. Applying the medicines inhibiting action of a miostatin it is possible to receive failure in operation of other elements of metabolic system. In other words, considering quite broad range of competence of this metabolic system, in addition to muscle growth there is a probability of numerous serious ghost effects from all systems of organs and fabrics.

Blockers of a miostatin in sports food

While in the scientific world there are ardent disputes and test works are actively conducted, the world of the sports industry actively makes absolutely safe and "effective" blockers of a miostatin.

Myo-Blast, according to the statement of the producer, contains the highest dose of the most powerful tool of the miostatin-corrective known as — Myozap CSP3.

Excerpt from the description:

Myozap CSP3 - a trade name patent structure for miostatin-protein neutralization. This extract is received from an exotic sea plant (Cystoseira canariensis) and at first was found during the scientific research conducted by researchers of biochemistry in Las Palmas University in Spain. As soon as you begin to neutralize miostanin, growth of new muscle cells begins. By means of this sports food, new cells of a muscle increase in the amount of and form new fibers of muscular tissue. Each new fiber, actually represents the potential for an additional new muscle, over what you already have. And these many new muscle fibers eventually are created in your body, giving you the chance to overcome the genetic threshold set miostatin.

Myostat, Myo-T12 and so forth have the similar description and the same active ingredient - Cystoseira canariensis.

"Attention" Despite these big words, these additives are absolutely inefficient. Now there is no additive which would influence exchange of a miostatin.

1. The researches conducted by Dzhordzhei Niffis, professor from Institute of National Health (the USA, the State of Ohio) have revealed that all qualities attributed to sports food on the basis of Cystoseira canariensis - no more, than the advertizing course. In the course of the experiment it has become clear that even in quantity in 50 times more recommended these additives haven't had any significant effect on growth of muscle bulk.

2. All modern antagonists of a miostatin of the proteinaceous nature, therefore they aren't accepted inside as in this case active agent would be inevitably destroyed by digestive enzymes.

Effective blockers of a miostatin

Creatine

In 2009 the research conducted by the Iranian scientists was published. They revealed that miostanin substantially is suppressed in case of additional acceptance of creatine.

Protein

Hulmi JJ and Tannerstedt J proved that the protein blocks synthesis of a miostatin in case of the systematic use by the training people.

Nicotine - the activator of a miostatin

"Attention" the Research, carried out by scientists of the Nottingham university, is established that activity of synthesis of muscle proteins at smokers was much lower, than at non-smoking. Besides, in an organism of fans of nicotine there is much higher than the level of protein of a miostatin and MAFbx enzyme. The first of them just detains muscle growth, and the second – splits proteins of muscles.