AC-262536 is a drug developed by
Acadia Pharmaceuticals
Acadia Pharmaceuticals Inc. is a biopharmaceutical company headquartered in Sorrento Valley, San Diego, Sorrento Valley, San Diego, San Diego, California.
Product development
Nuplazid, a drug developed by Acadia in the late 1990s, "was designe ...
which acts as a
selective androgen receptor modulator
Selective androgen receptor modulators (SARMs) are a class of drugs that tissue selectivity, selectively activate the androgen receptor in specific tissue (biology), tissues, promoting muscle and bone growth while having less effect on male re ...
(SARM). Chemically it possesses
endo-exo isomerism, with the endo form being the active form. It acts as a
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...
for the
androgen receptor
The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone, in th ...
with a
Ki of 5nM, and no significant affinity for any other receptors tested. In animal studies it produced a maximal effect of around 66% of the
levator ani
The levator ani is a broad, thin muscle group, situated on either side of the pelvis. It is formed from three muscle components: the pubococcygeus, the iliococcygeus, and the puborectalis.
It is attached to the inner surface of each side of the ...
muscle
Muscle is a soft tissue, one of the four basic types of animal tissue. There are three types of muscle tissue in vertebrates: skeletal muscle, cardiac muscle, and smooth muscle. Muscle tissue gives skeletal muscles the ability to muscle contra ...
weight increase of
testosterone
Testosterone is the primary male sex hormone and androgen in Male, males. In humans, testosterone plays a key role in the development of Male reproductive system, male reproductive tissues such as testicles and prostate, as well as promoting se ...
, but only around 27% of its maximal effect on
prostate gland
The prostate is an male accessory gland, accessory gland of the male reproductive system and a muscle-driven mechanical switch between urination and ejaculation. It is found in all male mammals. It differs between species anatomically, chemica ...
weight.
It is an
aniline
Aniline (From , meaning ' indigo shrub', and ''-ine'' indicating a derived substance) is an organic compound with the formula . Consisting of a phenyl group () attached to an amino group (), aniline is the simplest aromatic amine. It is an in ...
SARM related to
ACP-105
ACP-105 is a drug which acts as a selective androgen receptor modulator (SARM). It has been investigated for potential use in the treatment of age-related cognitive decline. The drug has been found to reduce anxiety-like behavior in a mouse mode ...
and
vosilasarm (RAD140).
References
Abandoned drugs
Naphthalenes
Nitriles
Secondary alcohols
Selective androgen receptor modulators
Tropanes
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