Org 27569

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Org 27569
Org27569 structure.png
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
Chemical and physical data
Formula C24H28ClN3O
Molar mass 409.951 g/mol
3D model (Jmol)
  (verify)

Org 27569 is a drug which acts as a potent and selective positive allosteric modulator of the cannabinoid CB1 receptor. Studies in vitro suggest that it 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. 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 antagonist of CB1 receptor function.[1]

See also[edit]

References[edit]

  1. ^ 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 (November 2005). "Allosteric modulation of the cannabinoid CB1 receptor". Molecular Pharmacology. 68 (5): 1484–95. doi:10.1124/mol.105.016162. PMID 16113085.