Org 27569

CB1

409.95

DMSO ：41 mg/mL (100 mM)

white

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.

ORG 27569 (3.2 and 5.6 mg/kg, i.p.) significantly attenuates cocaine associated cue-induced reinstatement, cocaine priming-induced reinstatement, methamphetamine associated cue-induced reinstatement and methamphetamine priming-induced reinstatement in rat. Org27569 (30 mg/kg, i.p.) produces CB1-independent hypophagic effects and does not affect the discriminative stimulus effects of anandamide (AEA). Org27569 (100 μg intracerebroventricularly) does not affect the pharmacologic effects of systemically administered CP55,940 compared with vehicle.

5-氯-3-乙基N-[2-(4-哌啶-1-基)苯基乙基]-1H-吲哚-2-甲酰胺

C₂₄H₂₈ClNO₃

868273-06-7