NESS-0327

From Wikipedia, the free encyclopedia
Jump to: navigation, search
NESS-0327
NESS-0327.png
Clinical data
Legal status
?
Identifiers
ATC code ?
PubChem CID 10435654
Chemical data
Formula C24H23Cl3N4O 
Mol. mass 489.824
 YesY (what is this?)  (verify)

NESS-0327 is a drug used in scientific research which acts as an extremely potent and selective antagonist of the cannabinoid receptor CB1. It is much more potent an antagonist, and more selective for the CB1 receptor over CB2, than the more commonly used ligand rimonabant, with a Ki at CB1 of 350fM (i.e. 0.00035nM) and a selectivity of over 60,000x for CB1 over CB2.[1] Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM[2] and 18.4nM[3]). Also unlike rimonabant, NESS-0327 does not appear to act as an inverse agonist at higher doses, instead being a purely neutral antagonist which blocks the CB1 receptor but does not produce any physiological effect of its own.[4]

See also[edit]

References[edit]

  1. ^ Ruiu S, Pinna GA, Marchese G, Mussinu JM, Saba P, Tambaro S, Casti P, Vargiu R, Pani L. Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor. Journal of Pharmacology and Experimental Therapeutics. 2003 Jul;306(1):363-70. PMID 12663689
  2. ^ A.R. Stoit, J.H.M. Lange, A.P. den Hartog, E. Ronken, K. Tipker, H.H. van Stuivenberg, J.A.R. Dijksman, H.C. Wals, C.G. Kruse, Chem. Pharm. Bull. 50 (2002) 1109-1113
  3. ^ Y. Zhang, J.P. Burgess, M. Brackeen, A. Gilliam, S.W. Mascarella, K. Page, H.H. Seltzman, B.F. Thomas, J. Med. Chem. 51 (2008) 3526-3539
  4. ^ Tambaro S, Mongeau R, Dessi C, Pani L, Ruiu S. Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors. European Journal of Pharmacology. 2005 Nov 21;525(1-3):150-3. PMID 16271359