SLV319

SLV319 has been used in trials studying the treatment of Obesity and Obesity and Type 2 Diabetes. (In Vitro) :Cannabinoid receptor 1 (CB1R) antagonists appear to be promising drugs for the treatment of obesity, however, serious side effects have hampered their clinical application. Ibipinabant is a new, potent [Ki (CB1) =7.8 nM] and selective [Ki (CB2) =7.943 nM] CB1 antagonist [pA2 for arachidonic acid release in CHO cells=9.9] with in vitro pharmacological characteristics similar to rimonabant including inverse agonism and brain penetrance. (In Vivo) : (±) -Ibipinabant ((±) -SLV319) (3 mg/kg) reduces unfasted glucose to a significantly greater degree than rimonabant at the same dose on days 17, 28 and 38. Chronic treatment with (±) -Ibipinabant ((±) -SLV319) significantly attenuates the progression of diabetes in ZDF rats, blunting the increase in blood glucose and HbA1c over time. Ibipinabant also reduces the hyperinsulinemia apparent at 6-8 weeks of age and attenuates the dramatic reduction in insulin levels observed 1-2 weeks later.