Org 27569 868273-06-7

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Molecular Weight:

409.95 Org 27569 is an allosteric modulator of Cannabinoid Cb1 Receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.

Biological Activity

Org 27569 is an allosteric modulator of CB1 cannabinoid receptor. It
significantly increases the binding of CB1 receptor agonist and causes a
significant decrease in specific binding of CB1 receptor inverse
agonist.


Org 27569 induces CB1 high affinity agonist binding, receptor internalization, and downstream ERK phosphorylation. The allosteric ligand Org 27569 promotes agonist binding to CB1, yet
blocks the agonist-induced conformational changes in TM6. Org 27569
traps the receptor in a distinct agonist-bound, but nonsignaling
conformational state.






Equilibrium Binding Assays


Binding assays are performed with the CB1 receptor agonist [3H]CP 55,940 (0.7 nM) and the CB1 receptor antagonist [3H]SR 141716A (1.2 nM), 1 mg/ml BSA and 50 mM Tris buffer containing 0.1 mM EDTA and 0.5 mM MgCl2,
pH 7.4, in a total assay volume of 500 μl. Binding is initiated by the
addition of mouse brain membranes (30 μg).


Assays are carried out at
37°C for 60 min before termination by addition of ice-cold wash buffer
(50 mM Tris buffer and 1 mg/ml BSA) and vacuum filtration using a
24-well sampling manifold and Whatman GF/B glass-fiber filters that have
been soaked in wash buffer at 4°C for 24 h. Each reaction tube is
washed five times with a 4-ml aliquot of buffer.


The filters are
oven-dried for 60 min and then placed in 5 ml of scintillation fluid,
and radioactivity is quantitated by liquid scintillation spectrometry.
Specific binding is defined as the difference between the binding that
occurred in the presence and absence of 1 μM concentrations of the
corresponding unlabeled ligand and is 70 to 80% of the total binding.

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Product Categories : GPCR & G Protein > Cannabinoid Receptor Inhibitor