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11.01.2020

NEP28, a SARM for your brain (and your muscles, of course)

Researchers from the Japanese chemical company Sumitomo Chemical [sumitomo-chem.co.jp] have developed a SARM that may not only counteract the breakdown of the muscles due to aging, but also the age-related deterioration of cognitive abilities. It is called NEP28.

Muscles
The researchers gave NEP28 in various doses to castrated male rats, and then looked at the effect of the compound on the prostate and the circular muscle levator ani. The extent to which those organs started to grow says something about the unwanted androgenic effects of NEP28 and the desired anabolic effects, respectively.

The Japanese did the same experiments with the androgenic testosterone metabolite DHT and methyltestosterone [MT]. They administered the substances with an osmotic pump, which they had implanted in their test animals.

NEP28 had an anabolic effect that, when administered at somewhat higher doses, was close to that of DHT and methyl testosterone. NEP28, on the other hand, hardly had any androgenic effects.

Brain
Androgens have an effect in the brain that gero-neurologists find very interesting. Androgens activate the enzyme neprilysin in brain tissue. This enzyme breaks down the amyloid-beta protein, that tends to accumulate in aging brain tissue.

In multiple forms of dementia, doctors find these accumulations in the brain, and so pharmacologists study drugs that break down amyloid beta - hoping that these drugs can slow down or prevent neurological aging.

In mice, DHT, methyl testosterone and NEP28 did exactly what they were supposed to do. These agents activated neprilysin and, as you see below, degraded the amyloid-beta plaques. Of course, this does not prove that NEP28 actually combats dementia.

Click on the figure below for a larger version.

Conclusion
"Our results indicate that androgen therapy with SARMs may be a very promising treatment method for not only diseases mainly targeted by current androgant herapy, but also neural diseases", write the researchers.

"SARMs having activity in brain are capable of improving various symptoms, including osteoporosis, sarcopenia, and neural diseases or cognition such as Alzheimer's disease simultaneously. Such children or SARMs certainly contribute to the enhancement of quality of life for many patients."

Critical comment
We, the ignorant compilers of this free web magazine, think that NEP28 will not be marketed. Perhaps an analogue of NEP28 offers perspectives, but NEP28 itself does not seem interesting, despite the tempting perspective that the researchers outline above.

The dose required for a significant anabolic effect is very high. The human equivalent of the highest dose of NEP28 that the Japanese gave to their lab animals amounts to 250-300 milligrams per day...

Source:
Eur J Pharmacol. 2013;720(1-3):107-14.

More:
MK-4541: a SARM that makes muscles stronger and kills cancer cells 24.03.2019
S42, the Japanese fat loss SARM 05.02.2019
The anabolic effect of GSK20881078: human study 31.10.2018
GSK2881078 - SARM star rising 30.01.2018

Archives:
Anabolic Substances
Preventing Dementia
SARMs

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