ness-0327とは 意味・読み方・使い方

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.. Independently, two other groups have described only modest nanomolar CB₁ affinity for this compound (125nM and 18.4nM). 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.