NESS 0327

NESS 0327 is an extremely potent cannabinoid receptor antagonist, selective for the CB1 receptor (K_i = 0.35 pM) over the CB2 receptor (K_i = 21 nM). It is more potent and selective for the CB1 receptor than rimonabant, one of the first discovered CB receptor antagonists. 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. Unlike rimonabant, NESS 0327 does not act as a CB1 receptor inverse agonist at higher concentrations, nor does it produce any physiological effects of its own.