产品描述:
LH 21 is a 1,2,4-triazole that acts as a cannabimimetic. It has a relatively low-affinity for the central cannabinoid (CB1) receptor (Ki = 855 nM).{19248} However, it interferes, at low nanomolar concentrations, with the action of the potent CB1 agonist WIN 55,212-2 on murine vas deferens, suggesting that LH 21 acts as a silent CB1 antagonist.{19248} Consistent with this interpretation, LH 21 diminishes the in vivo effects of WIN 55,212-2 on standard CB tetrad responses in mice and reduces food intake and body weight gain in obese Zucker rats.{19248,19238,19239} However, in CHO cells overexpressing CB1, LH 21 is able to elevate cAMP, suggesting that, in this model, it acts as an inverse agonist of CB1.{19237} Furthermore, LH 21 suppresses food intake and body weight gain in both wild-type and CB1 receptor knockout mice, indicating that this receptor is not necessary for these effects.{19237}