Ibipinabant

Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a K_i of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (K_i=7943 nM). Ibipinabant can be used for the research of obesity and diabetic^[1][2][3]. In Vitro: SLV319?displaces the specific CP-55940 (CB agonist) binding in CHO cells stably transfected with human CB1 receptor, with a K_i of 7.8 nM^[1].
SLV319 concentration dependently antagonizes WIN-55212 (CB1 agonist)-induced arachidonic acid release in CHO cells, with a pA2 of 9.9^[1]. In Vivo: SLV319?(3 mg/kg/day; p.o. for 28 d) reduces the food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obesity (DIO) mice^[2].
SLV319 (3 mg/kg/day, p.o. for 28 d) reverses the HFD-induced increase in adipose tissue leptin mRNA^[2].
SLV319 (3-10 mg/kg; daily oral gavage for 56 d) has weight loss-independent antidiabetic effects and attenuates β-cell loss in a rat model of progressive β-cell dysfunction^[3].
SLV319 (oral administration) antagonizes CB agonist (CP55940) induced hypotension in rats and hypothermia in mice, with an ED₅₀ of 5.5 and 3 mg/kg, respectively^[1].