Drinabant Chemical Properties

Boiling point:

581.7±60.0 °C(Predicted)

Density 

1.458

storage temp. 

Store at -20°C

solubility 

≤0.15mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide

form 

crystalline solid

pka

5.44±0.10(Predicted)

color 

White to off-white

Drinabant Usage And Synthesis

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.

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.

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