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Description: Org 27569 is a novel, potent and selective allosteric modulator of cannabinoid CB1 receptor, it induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity. Org 27569 binds to a regulatory site on the CB1 receptor target, causing a conformational change that increases the binding affinity of CB1 agonists such as CP 55, 940, while decreasing the binding affinity of CB1 antagonists or inverse agonists such as rimonabant.
References: Mol Pharmacol. 2005 Nov; 68(5):1484-95; J Biol Chem. 2012 Apr 6; 287(15):12070-82.
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