SR9009, also known as Stenabolic, is a research drug that was developed by professor Thomas Burris of the
Scripps Research Institute
Scripps Research is a nonprofit American medical research facility that focuses on research and education in the biomedical sciences. Headquartered in San Diego, California, the institute has over 170 laboratories employing 2,100 scientists, tec ...
as an
agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
of
Rev-ErbA
The Rev-Erb proteins are members of the Nuclear receptor, nuclear receptor (NR) superfamily of Transcription factor, intracellular transcription factors and key regulatory components of the circadian clock. There are two forms of the receptor ...
(i.e., increases the constitutive
repression of
genes regulated by Rev-ErbA)
with a half-maximum inhibitory concentration (
IC50) = 670 nM for
Rev-ErbAα and IC
50 = 800 nM for
Rev-ErbAβ.
In an animal study, some of its effects were found to be independent of REV-ERB with an unknown
mechanism of action
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical Drug interaction, interaction through which a Medication, drug substance produces its pharmacological effect. A mechanism of action usually includes mention o ...
.
Activation of Rev-ErbA-α by SR9009 in mice increases exercise capacity by increasing
mitochondria
A mitochondrion () is an organelle found in the cells of most eukaryotes, such as animals, plants and fungi. Mitochondria have a double membrane structure and use aerobic respiration to generate adenosine triphosphate (ATP), which is us ...
counts in
skeletal muscle
Skeletal muscle (commonly referred to as muscle) is one of the three types of vertebrate muscle tissue, the others being cardiac muscle and smooth muscle. They are part of the somatic nervous system, voluntary muscular system and typically are a ...
.
Abuse of SR9009 has been reported within the bodybuilding community, resulting in SR9009 being placed on the
World Anti-Doping Agency
The World Anti-Doping Agency (WADA; , AMA) is an international organization co-founded by the governments of over 140 nations along with the International Olympic Committee based in Canada to promote, coordinate, and monitor the fight against d ...
list of
prohibited drugs. SR9009 and the related
SR9011 drug are described as "Hormone and Metabolic Modulators".
See also
*
GSK4112
GSK-4112 is an experimental drug that was developed by GlaxoSmithKline as an agonist of Rev-ErbAα. It is used for studying regulation of the circadian rhythm and its influence on diverse processes such as adipogenesis, regulation of bone densit ...
*
GW501516
GW501516 (also known as GW-501,516, GW1516, GSK-516, cardarine, and on the black market as endurobol) is a PPARδ receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. It entered ...
*
SR8278
SR-8278 is an experimental drug that was developed as an antagonist of Rev-ErbAα. It has been used to demonstrate potential applications of Rev-ErbAα antagonists in the treatment of conditions such as Duchenne muscular dystrophy and Alzheimer' ...
*
SR9011
References
Tertiary amines
Benzene derivatives
Experimental drugs
Thiophenes
Drugs with unknown mechanisms of action
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