CVT-10216 counteracted anxiety in all models except that produced by the 5-HT(2C) agonist, mCPP. CVT-10216 exhibited both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety. CVT-10216 increases acetaldehyde after alcohol gavage and inhibits 2-bottle choice alcohol intake in heavy drinking rodents, including deprivation-induced drinking. CVT-10216 also prevents operant self-administration and eliminates cue-induced reinstatement of alcohol seeking even when alcohol is not available (i.e., no acetaldehyde). CVT-10216 prevents alcohol-induced increases in NAc DA without changing basal levels. CVT-10216 does not show rewarding or aversive properties in the CPP paradigm at therapeutic doses.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
A selective ALDH-2 inhibitor reduces anxiety in rats.
Overstreet DH, et al. Pharmacol Biochem Behav. 2009 Dec;94(2):255-61. PMID: 19747934.
Suppression of heavy drinking and alcohol seeking by a selective ALDH-2 inhibitor.
Arolfo MP, et al. Alcohol Clin Exp Res. 2009 Nov;33(11):1935-44. PMID: 19673742.
CVT-10216 selectively suppresses binge eating of palatable foods and attenuates dopamine release in the accumbens of rats
Miriam E Bocarsly, et al. The FASEB Journal. 2012;26:1012.3.
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