Drinabant

Description

The central cannabinoid (CB₁) receptor is a G protein-coupled receptor that is widely distributed in the central nervous system and several peripheral tissues and binds the active component of cannabis, Δ⁹-tetrahydrocannabinol. Signaling through the CB₁ receptor is implicated in attentional and working memory deficits as well as obesity. AVE-1625 is a highly potent, selective antagonist for the CB₁ receptor with K_i values of 0.16-0.44 nM. At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks. At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents.

Uses

AVE-1625 is a selective antagonist for the CB1 receptor.

in vivo

IC 50

hCB1-R: 25 nM (IC₅₀); rCB1-R: 10 nM (IC₅₀); CB2: 10000 nM (IC₅₀)

storage

Store at -20°C

References

[1] borowsky b, stevens r, mark b, et al. ave1625, a cannabinoid cbi antagonist, as a co-treatment for schizophrenia: improvement in cognitive function and reduction of antipsychotic-side effects in animal models[c]//neuropsychopharmacology. macmillan building, 4 crinan st, london n1 9xw, england: nature publishing group, 2005, 30: s116-s117.
[2] herkenham m, lynn a b, little m d, et al. cannabinoid receptor localization in brain[j]. proceedings of the national academy of sciences, 1990, 87(5): 1932-1936.
[3] herling a w, gossel m, haschke g, et al. cb1 receptor antagonist ave1625 affects primarily metabolic parameters independently of reduced food intake in wistar rats[j]. american journal of physiology-endocrinology and metabolism, 2007, 293(3): e826-e832.