Org 27569: Difference between revisions

| verifiedrevid = 426277049

| routes_of_administration =

| excretion =

| molecular_weight = 409.951 g/mol

| smiles = CCc1c2cc(Cl)ccc2nc1C(=O)NCCc3ccc(cc3)N4CCCCC4

| StdInChI_Ref = {{stdinchicite|correct|chemspider}}

'''Org 27569''' is a drug which acts as a potent and selective [[allosteric modulator]] of the [[cannabinoid]] [[Cannabinoid receptor 1|CB₁]] [[Receptor (biochemistry)|receptor]]. Studies ''in vitro'' suggest that it binds to a regulatory site on the CB₁ receptor target, causing a conformational change that increases the [[Dissociation constant#Protein-ligand binding|binding affinity]] of CB₁ agonists such as [[CP 55,940]], while decreasing the binding affinity of CB₁ antagonists or inverse agonists such as [[rimonabant]]. However while Org 27569 increases the ability of CB₁ agonists to bind to the receptor, it decreases their efficacy at stimulating [[second messenger]] signalling once bound, and so in practice behaves as an insurmountable [[Receptor antagonist|antagonist]] of CB₁ receptor function.<ref name="pmid16113085">{{cite journal |author=Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G, Westwood P, Marrs J, Thomson F, Cowley P, Christopoulos A, Pertwee RG, Ross RA |title=Allosteric modulation of the cannabinoid CB1 receptor |journal=Molecular Pharmacology |volume=68 |issue=5 |pages=1484–95 |year=2005 |month=November |pmid=16113085 |doi=10.1124/mol.105.016162 |url=}}</ref>