NESS 0327

NESS 0327 is an extremely potent cannabinoid (CB) receptor antagonist with high selectivity for the CB1 receptor compared to the CB2 receptor with Ki values of 0.35 pM and 21 nM, respectively.{11553} It is a much more potent antagonist and more selective for the CB1 receptor compared to SR 141716A (rimonabant). At nM concentrations NESS 0327 competitively inhibits the binding of the synthetic CB agonist WIN 55,212-2 in isolated rat cerebella membranes and murine vas deferens.{11553,15795} Unlike SR 141716A, NESS 0327 at higher doses does not act as a CB1 receptor inverse agonist and does not produce any physiological effects of its own.{11553,15795}