SR-144,528
SR-144,528 is a drug that acts as a potent and selective antagonist for the CB2 receptor, and was discovered by Sanofi-Aventis. It is used in scientific research for distinguishing the actions of the CB1 receptor and CB2 receptors, and has been used to demonstrate that many cannabinoid effects previously thought to be produced by CB1 receptors could also involve CB2 receptors.
Discovery
Sanofi-Aventis, a French multinational pharmaceutical company, discovered SR-144,528. The drug was developed as part of the company's research into treatments for various conditions, including pain, obesity, and neurodegenerative disorders.
Mechanism of Action
SR-144,528 acts as a potent and selective antagonist for the CB2 receptor. This means it blocks the action of cannabinoids at the CB2 receptor, preventing them from producing their typical effects. This is in contrast to agonists, which activate the receptor and produce a response.
Use in Research
SR-144,528 is used in scientific research to distinguish the actions of the CB1 and CB2 receptors. This is important because the two receptors are very similar and are both activated by cannabinoids. By using SR-144,528, researchers can block the CB2 receptor and see what effects are still produced by the CB1 receptor.
In addition, SR-144,528 has been used to demonstrate that many cannabinoid effects previously thought to be produced by CB1 receptors could also involve CB2 receptors. This has implications for our understanding of the endocannabinoid system and how it can be targeted for therapeutic purposes.
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Contributors: Prab R. Tumpati, MD