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09.07.2020

Animal study: lean or fat, old or young, Bay 60-6583 improves your body composition

'Oh dear', we thought when we read the article that German pharmacologist Thorsten Gnad, of the University of Bonn, published in Cell Metabolism. 'This stuff will hit the market as a research chemical. Just wait.' The substance we are talking about? Bay 60-6583.

Bay 60-6583
Bay 60-6583 is officially named 2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)-phenyl]-pyridin-2-ylsulfanyl]-acetamide. The substance activates the A2B adenosine receptor, and doctors hope the compound is a medicine for arteriosclerosis and other vascular disorders. [Purinergic Signal. 2008 Dec;4(4):287-303.]

Thorsten Gnad suspects that substances like Bay 60-6583 can do much more than repair damaged blood vessels. The A2B receptor is mainly present in brown adipose tissue and muscle, and Gnad's animal studies show that when that receptor is turned on by Bay 60-6583, muscle tissues and calorie consumption increase.

In his publication, Gnad tells that he gave young, middle-aged mice and elderly lab mice Bay 60-6583 daily for 4 weeks. He injected the substance directly into their small intestines. That method of administration imitates to some extent the effects of oral administration. We estimate that if the mice had been adult humans, they would have received about 15 milligrams of Bay 60-6583 per day.

The animals became more muscular and stronger. In fact, it seems that Bay 60-6583 may be a drug for sarcopenia.

Slimmer
In another series of animal studies, the researchers fattened mice by feeding them extra fat [HFD]. If the animals also received Bay 60-6583, they became less fat and their oxygen consumption increased. You can see this above.

Safe?
We honestly don't know anything about the safety of this substance. However, the researchers say nothing about side effects in their publication. In a press release, study leader Alexander Pfeifer also says that the researchers have not found them. [sciencedaily.com June 25, 2020]

"We found no signs of adverse reactions in mice", says Pfeifer. "However, the meaningfulness of the results is, of course, also limited on this matter."

Conclusion
"Our data demonstrate that the adenosine A2B signaling pathway plays a central role in maintaining skeletal muscle mass and function", the researchers summarize in the last paragraphs of their publication.

"Stimulation of A2B counteracted age-related and obesity-associated sarcopenia and restored skeletal muscle function and mass to juvenile levels. In parallel, A2B activation was also relieving age- and obesity-related decline in brow adipose tissue function and induced browning of white adipose tissue."

"Together, our data indicate that targeting this single receptor might be a novel, holistic approach toward healthy aging and metabolic balance."

Source:
Cell Metab. 2020 Jun 22;S1550-4131(20)30307-7. doi: 10.1016/j.cmet.2020.06.006. Online ahead of print.

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