SR144528 is a drug that acts as a potent and highly selective
CB2 receptor
Receptor may refer to:
*Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a n ...
inverse agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
A neutral antagonist has no activity in the absence of an agonist or inverse ago ...
, with a
Ki of 0.6 nM at CB
2 and 400 nM at the related CB
1 receptor.
It is used in scientific research for investigating the function of the CB
2 receptor,
as well as for studying the effects of CB
1 receptors in isolation, as few CB
1 agonists that do not also show significant activity as CB
2 agonists are available.
It has also been found to be an inhibitor of
sterol O-acyltransferase
Sterol O-acyltransferase (also called Acyl-CoA cholesterol acyltransferase, Acyl-CoA cholesterin acyltransferase or simply ACAT) is an intracellular protein located in the endoplasmic reticulum that forms cholesteryl esters from cholesterol. ...
, an effect that appears to be independent from its action on CB
2 receptors.
See also
*
NESS-040C5
*
Rimonabant
Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) is an anorectic antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in t ...
*
MN-25
MN-25 (UR-12) is a drug invented by Bristol-Myers Squibb, that acts as a reasonably selective agonist of peripheral cannabinoid receptors. It has moderate affinity for CB2 receptors with a ''K''i of 11 nM, but 22x lower affinity for the p ...
References
Cannabinoids
Chloroarenes
Pyrazolecarboxamides
{{cannabinoid-stub