Org 27569 is a drug which acts as a potent and selective negative allosteric modulator of the cannabinoidCB1receptor. 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]
27569, drug, which, acts, potent, selective, negative, allosteric, modulator, cannabinoid, receptor, studies, vitro, suggest, that, binds, regulatory, site, receptor, target, causing, conformational, change, that, increases, binding, affinity, agonists, such, . Org 27569 is a drug which acts as a potent and selective negative 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 Org 27569IdentifiersIUPAC name 5 chloro 3 ethyl 1H indole 2 carboxylic acid 2 4 piperidin 1 yl phenyl ethyl amideCAS Number868273 06 7 YPubChem CID44828492IUPHAR BPS7851ChemSpider22369629 YUNII7YW2S3Z2CBCompTox Dashboard EPA DTXSID00660764Chemical and physical dataFormulaC 24H 28Cl N 3OMolar mass409 96 g mol 13D model JSmol Interactive imageSMILES CCc1c2cc Cl ccc2 nH c1C O NCCc3ccc cc3 N4CCCCC4InChI InChI 1S C24H28ClN3O c1 2 20 21 16 18 25 8 11 22 21 27 23 20 24 29 26 13 12 17 6 9 19 10 7 17 28 14 4 3 5 15 28 h6 11 16 27H 2 5 12 15H2 1H3 H 26 29 Key AHFZDNYNXFMRFQ UHFFFAOYSA N Y verify See also editGAT100 PSNCBAM 1 ZCZ 011References edit 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 S2CID 17648541 nbsp This cannabinoid related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Org 27569 amp oldid 1188796829, wikipedia, wiki, book, books, library,
